Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H25ClO7.C5H7NO3 |
Molecular Weight | 565.997 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)[C@@H]1CCC(=O)N1.CCOC2=CC=C(CC3=C(Cl)C=CC(=C3)[C@]45OC[C@](CO)(O4)[C@@H](O)[C@H](O)[C@H]5O)C=C2
InChI
InChIKey=YHIUPZFKHZTLSH-LXYIGGQGSA-N
InChI=1S/C22H25ClO7.C5H7NO3/c1-2-28-16-6-3-13(4-7-16)9-14-10-15(5-8-17(14)23)22-20(27)18(25)19(26)21(11-24,30-22)12-29-22;7-4-2-1-3(6-4)5(8)9/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3;3H,1-2H2,(H,6,7)(H,8,9)/t18-,19-,20+,21-,22-;3-/m00/s1
Molecular Formula | C5H7NO3 |
Molecular Weight | 129.114 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C22H25ClO7 |
Molecular Weight | 436.883 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Ertugliflozin (PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor incorporating a unique dioxa-bicyclo[3.2.1]octane (bridged ketal) ring system. SGLT2 has become an important therapeutic target and several SGLT2-selective inhibitors are either approved or in clinical development for the management of blood glucose in patients with type 2 diabetes. Ertugliflozin demonstrated robust urinary glucose excretion in rats and an excellent preclinical safety profile. It was announced that FDA and EMA filing acceptances of three marketing applications for ertugliflozin-containing medicines for adults with type 2 diabetes.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21449606
Curator's Comment: # Pfizer, Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3884 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21449606 |
0.877 nM [IC50] | ||
Target ID: CHEMBL4979 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21449606 |
1960.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ERTUGLIFLOZIN Approved UseUnknown |
|||
Primary | STEGLATRO Approved UseSTEGLATRO™ is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Launch Date2017 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
81.3 ng/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ERTUGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
398 ng × h/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ERTUGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.6 h |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ERTUGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.4% |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ERTUGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Disc. AE: Hyperglycaemia, Glomerular filtration rate decreased... AEs leading to discontinuation/dose reduction: Hyperglycaemia (0.5%) Sources: Page: p. 97Glomerular filtration rate decreased (0.4%) Balanoposthitis (0.1%) Urinary tract infection (0.2%) Vulvovaginal mycotic infection (0.1%) Acute kidney injury (0.1%) Pollakiuria (0.2%) Vulvovaginal pruritus (0.1%) Vulvovaginal candidiasis (0.2%) Diarrhoea (0.1%) Nausea (0.1%) Weight decreased (0.1%) Acute myocardial infarction (0.1%) Blood creatinine increased (0.1%) Dysuria (0.1%) Genital candidiasis (0.1%) Hypoglycaemia (0.1%) Insomnia (0.1%) Non-cardiac chest pain (0.1%) Polyuria (0.1%) Pruritus genital (0.1%) Rash (0.1%) Incontinence urinary (0.1%) Abdominal pain (0.1%) Alopecia (0.1%) Arthralgia (0.1%) Asthma (0.1%) Benign ovarian tumor (0.1%) Cellulite (0.1%) Cholelithiasis (0.1%) Colon cancer (0.1%) Dermatitis allergic (0.1%) Diabetic ketoacidosis (0.1%) Dry mouth (0.1%) Dysphonia (0.1%) Endometrial adenocarcinoma (0.1%) Fatigue (0.1%) Haematuria (0.1%) Headache (0.1%) Jaundice cholestatic (0.1%) Liver disorder (0.1%) Malaise (0.1%) Metabolic acidosis (0.1%) Mood swings (0.1%) Nightmare (0.1%) Pancreatic neoplasm (0.1%) Penile pain (0.1%) Peripheral ischaemia (0.1%) Peripheral swelling (0.1%) Plasma cell myeloma (0.1%) Prurigo (0.1%) Rash maculo-papular (0.1%) Septic shock (0.1%) Vision blurred (0.1%) Vulvovaginitis (0.1%) |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Disc. AE: Hyperglycaemia, Glomerular filtration rate decreased... AEs leading to discontinuation/dose reduction: Hyperglycaemia (0.3%) Sources: Page: p. 97Glomerular filtration rate decreased (0.1%) Balanoposthitis (0.3%) Urinary tract infection (0.1%) Vulvovaginal mycotic infection (0.2%) Acute kidney injury (0.1%) Pollakiuria (0.1%) Vulvovaginal pruritus (0.1%) Vulvovaginal candidiasis (0.1%) Diarrhoea (0.1%) Dizziness (0.2%) Nausea (0.1%) Weight decreased (0.1%) Abdominal pain upper (0.1%) Acute myocardial infarction (0.1%) Blood creatinine increased (0.1%) Dysuria (0.1%) Genital candidiasis (0.1%) Hypoglycaemia (0.1%) Insomnia (0.1%) Non-cardiac chest pain (0.1%) Polyuria (0.1%) Pruritus genital (0.1%) Rash (0.1%) Rheumatoid arthritis (0.1%) Adenocarcinoma gastric (0.1%) Alanine aminotransferase increased (0.1%) Aspartate aminotransferase increased (0.1%) Asthenia (0.1%) Blood glucose increased (0.1%) Breast cancer (0.1%) Cerebral infarction (0.1%) Cerebrovascular accident (0.1%) Coronary artery disease (0.1%) Diabetic foot (0.1%) Diabetic neuropathy (0.1%) Dyslipidaemia (0.1%) Face injury (0.1%) Facial paralysis (0.1%) Fungal skin infection (0.1%) Genital infection (0.1%) Head discomfort (0.1%) Hepatocellular injury (0.1%) Humerus fracture (0.1%) Hunger (0.1%) Hyperchlorhydria (0.1%) Musculoskeletal pain (0.1%) Myocardial infarction (0.1%) Nephropathy (0.1%) Obesity (0.1%) Oral candidiasis (0.1%) Osteomyelitis acute (0.1%) Pain in extremity (0.1%) Acute pancreatitis (0.1%) Pyelonephritis (0.1%) Pyelonephritis acute (0.1%) Thirst (0.1%) Urinary retention (0.1%) Urogenital infection fungal (0.1%) Vaginal infection (0.1%) |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Other AEs: Acute myocardial infarction, Haemorrhagic stroke... Other AEs: Acute myocardial infarction (grade 5, 0.18%) Sources: Page: p.84Haemorrhagic stroke (grade 5, 0.06%) Ischaemic stroke (grade 5, 0.06%) Septic shock (grade 5, 0.06%) Plasma cell myeloma (grade 5, 0.06%) |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Other AEs: Acute myocardial infarction, Cardiac death... Other AEs: Acute myocardial infarction (grade 5, 0.06%) Sources: Page: p.84Cardiac death (grade 5, 0.17%) Multiple organ dysfunction syndrome (grade 5, 0.06%) Pneumonia (grade 5, 0.06%) Chronic obstructive pulmonary disease (grade 5, 0.06%) Depression (grade 5, 0.06%) |
100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: |
healthy |
|
300 mg single, oral Highest studied dose |
healthy |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Abdominal pain | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Acute kidney injury | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Acute myocardial infarction | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Alopecia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Arthralgia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Asthma | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Balanoposthitis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Benign ovarian tumor | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Blood creatinine increased | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Cellulite | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Cholelithiasis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Colon cancer | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Dermatitis allergic | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Diabetic ketoacidosis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Diarrhoea | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Dry mouth | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Dysphonia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Dysuria | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Endometrial adenocarcinoma | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Fatigue | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Genital candidiasis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Haematuria | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Headache | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Hypoglycaemia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Incontinence urinary | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Insomnia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Jaundice cholestatic | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Liver disorder | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Malaise | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Metabolic acidosis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Mood swings | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Nausea | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Nightmare | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Non-cardiac chest pain | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Pancreatic neoplasm | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Penile pain | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Peripheral ischaemia | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Peripheral swelling | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Plasma cell myeloma | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Polyuria | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Prurigo | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Pruritus genital | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Rash maculo-papular | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Rash | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Septic shock | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Vision blurred | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Vulvovaginal mycotic infection | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Vulvovaginal pruritus | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Vulvovaginitis | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Weight decreased | 0.1% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Pollakiuria | 0.2% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Urinary tract infection | 0.2% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Vulvovaginal candidiasis | 0.2% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Glomerular filtration rate decreased | 0.4% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Hyperglycaemia | 0.5% Disc. AE |
15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1693 Health Status: unhealthy Age Group: > 65 years Population Size: 1693 Sources: Page: p. 97 |
Abdominal pain upper | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Acute kidney injury | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Acute myocardial infarction | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Acute pancreatitis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Adenocarcinoma gastric | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Alanine aminotransferase increased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Aspartate aminotransferase increased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Asthenia | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Blood creatinine increased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Blood glucose increased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Breast cancer | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Cerebral infarction | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Cerebrovascular accident | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Coronary artery disease | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Diabetic foot | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Diabetic neuropathy | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Diarrhoea | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Dyslipidaemia | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Dysuria | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Face injury | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Facial paralysis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Fungal skin infection | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Genital candidiasis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Genital infection | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Glomerular filtration rate decreased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Head discomfort | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Hepatocellular injury | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Humerus fracture | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Hunger | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Hyperchlorhydria | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Hypoglycaemia | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Insomnia | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Musculoskeletal pain | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Myocardial infarction | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Nausea | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Nephropathy | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Non-cardiac chest pain | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Obesity | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Oral candidiasis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Osteomyelitis acute | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Pain in extremity | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Pollakiuria | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Polyuria | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Pruritus genital | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Pyelonephritis acute | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Pyelonephritis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Rash | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Rheumatoid arthritis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Thirst | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Urinary retention | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Urinary tract infection | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Urogenital infection fungal | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Vaginal infection | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Vulvovaginal candidiasis | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Vulvovaginal pruritus | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Weight decreased | 0.1% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Dizziness | 0.2% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Vulvovaginal mycotic infection | 0.2% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Balanoposthitis | 0.3% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Hyperglycaemia | 0.3% Disc. AE |
5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p. 97 |
unhealthy, > 65 years n = 1716 Health Status: unhealthy Age Group: > 65 years Population Size: 1716 Sources: Page: p. 97 |
Haemorrhagic stroke | grade 5, 0.06% | 15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Ischaemic stroke | grade 5, 0.06% | 15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Plasma cell myeloma | grade 5, 0.06% | 15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Septic shock | grade 5, 0.06% | 15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Acute myocardial infarction | grade 5, 0.18% | 15 mg 1 times / day steady, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1693 Health Status: unhealthy Age Group: adult Population Size: 1693 Sources: Page: p.84 |
Acute myocardial infarction | grade 5, 0.06% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Chronic obstructive pulmonary disease | grade 5, 0.06% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Depression | grade 5, 0.06% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Multiple organ dysfunction syndrome | grade 5, 0.06% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Pneumonia | grade 5, 0.06% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Cardiac death | grade 5, 0.17% | 5 mg 1 times / day steady, oral (starting) Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: Page: p.84 |
unhealthy, adult n = 1716 Health Status: unhealthy Age Group: adult Population Size: 1716 Sources: Page: p.84 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 41-42, 91-92 |
no [IC50 917 uM] | no (co-administration study) Comment: Ki = 917 mcM; Not meaningfully inhibit at clinically relevant concentrations; Coadministration of ertugliflozin (15 mg SD) decreased metformin (OCT2 substrate, 1000 mg SD) Cmax by 6% and increased AUCinf by 0.94%. There are no meaningful difference in the PK of metformin when it is administered with ertugliflozin, as compared to single dose of metformin alone. Page: (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 41-42, 91-92 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=186 Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=186 Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=186 Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=186 Page: (IND106447) 21, (NDA209803) 10, 27, 206, 207, (NDA209805) 11, 44, (NDA209806) 11, 44 |
no [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=186 Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [IC50 >30 uM] | |||
Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 43-44, 94-95 |
no [IC50 >30 uM] | no (co-administration study) Comment: Ki > 15 mcM; Not a reversible or time-dependent inhibitor (humna liver microsomes), IC50 value (>30 mcM) is at least 50-fold higher than clinical ertugliflozin Cmax concentrations (0.6 mcM).; Coadministration of ertugliflozin (15 mg SD) decreased glimepiride (1 mg SD) Cmax by 2.61% and increased AUCinf by 9.80%. There are no meaningful difference in the PK of glimepiride when it is administered with ertugliflozin, as compared to single dose of glimepiride alone. Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 43-44, 94-95 |
||
Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207 (NDA209805) 11, 44, (NDA209806) 11, 44, (ClinPharm) 39-40, 89-90, 45-46, 96-98 |
no [IC50 >30 uM] | no (co-administration study) Comment: Ki > 15 mcM; Not a reversible or time-dependent inhibitor (humna liver microsomes), IC50 value (>30 mcM) is at least 50-fold higher than clinical ertugliflozin Cmax concentrations (0.6 mcM)., Coadministration of ertugliflozin (15 mg SD) increased sitagliptin (CYP3A4 substarte, 100 mg SD) Cmax by 1.68% and AUCinf by 1.67%. There are no meaningful difference in the PK of sitagliptin when it is administered with ertugliflozin, as compared to single dose of sitagliptin alone., Coadministration of ertugliflozin (15 mg SD) increased simvastatin (CYP3A substrate, 40 mg SD) Cmax by 19.05% and AUCinf by 23.83%. There are no meaningful difference in the PK of glimepiride when it is administered with ertugliflozin, as compared to single dose of simvastatin alone. Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207 (NDA209805) 11, 44, (NDA209806) 11, 44, (ClinPharm) 39-40, 89-90, 45-46, 96-98 |
||
Page: (IND106447) 21, (NDA209803) 29, (ClinPharm) 45-46, 96-98 |
no [Ki >15 uM] | no (co-administration study) Comment: Ki > 15 mcM; Not a reversible or time-dependent inhibitor (humna liver microsomes); Coadministration of ertugliflozin (15 mg SD) increased simvastatin (CYP3A substrate, 40 mg SD) Cmax by 19.05% and AUCinf by 23.83%. There are no meaningful difference in the PK of glimepiride when it is administered with ertugliflozin, as compared to single dose of simvastatin alone. Page: (IND106447) 21, (NDA209803) 29, (ClinPharm) 45-46, 96-98 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 11, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [Ki >250 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [Ki >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [Ki >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no [Ki >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (IND122329) 15, (IND106447) 21, (NDA209803) 27, 29, 206, 207, 210(NDA209803) 10, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (NDA209803) 10, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (IND106447) 21, (NDA209803) 27, 29, 206, 207, 210, (NDA209803) 10, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (IND106447) 21, (NDA209803) 11, 28, 29, 207, 210 |
weak [IC50 140.7 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44 |
weak [IC50 176 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (IND106447) 21, (NDA209803) 11, 28, 29, 207, 210 |
weak [IC50 35.4 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
weak [IC50 39 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44 |
weak [IC50 45 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 28, 29, 210 |
weak [IC50 53 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (IND106447) 21, (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44 |
weak [IC50 70 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=187 Page: (NDA209803) 28, 29, 210 |
weak [Inhibition 100 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=12 Page: (NDA209803) 10, 29, (NDA209805) 11, 43, (NDA209806) 11, 43, (NDA ClinPharm) 47-48, 99-100 |
major | yes (co-administration study) Comment: Coadministration of ertugliflozin (15 mg SD) with multiple doses of rifampicin (an inducer of UGT and CYP emzymes, 600 mg QD) decreased ertugliflozin Cmax by 15.38% and AUCinf by 38.84%. Mean terminal t1/2 was 12.3 hr for ertugliflozin administered alone compared to 9.2 hr for ertugliflozin coadministered with rifampicin. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=12 Page: (NDA209803) 10, 29, (NDA209805) 11, 43, (NDA209806) 11, 43, (NDA ClinPharm) 47-48, 99-100 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=12 Page: (NDA209803) 10, 29, (NDA209805) 11, 43, (NDA209806) 11, 43 |
major | yes (co-administration study) Comment: Coadministration of ertugliflozin (15 mg SD) with multiple doses of rifampicin (an inducer of UGT and CYP emzymes, 600 mg QD) decreased ertugliflozin Cmax by 15.38% and AUCinf by 38.84%. Mean terminal t1/2 was 12.3 hr for ertugliflozin administered alone compared to 9.2 hr for ertugliflozin coadministered with rifampicin. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=12 Page: (NDA209803) 10, 29, (NDA209805) 11, 43, (NDA209806) 11, 43 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=12 Page: (NDA209803) 29, (NDA209805) 11, (NDA209806) 11 |
minor | |||
Page: (NDA209803) 29, (NDA209805) 11, (NDA209806) 11, (ClinPharm) 39, 89-90, 44-45, 96-98 |
minor | yes (co-administration study) Comment: Coadministration of ertugliflozin (15 mg SD) with multiple doses of rifampicin (an inducer of UGT and CYP emzymes, 600 mg QD) decreased ertugliflozin Cmax by 15.38% and AUCinf by 38.84%. Mean terminal t1/2 was 12.3 hr for ertugliflozin administered alone compared to 9.2 hr for ertugliflozin coadministered with rifampicin., Coadministration of sitagliptin (metabolized by CYP3A4, 100 mg SD) decreased Cmax of ertugliflozin (15 mg SD) by 1.82% and increased AUCinf by 2.27%. There are no meaningful difference in the PK of ertugliflozin when it is administered with sitagliptin, as compared to single dose of ertugliflozin alone., Coadministration of simvastatin (CYP3A substrate, 40 mg SD) increased Cmax of ertugliflozin (15 mg SD) by 5.16% and AUCinf by 2.40%. There are no meaningful difference in the PK of ertugliflozin when it is administered with simvastatin, as compared to single dose of ertugliflozin alone. Page: (NDA209803) 29, (NDA209805) 11, (NDA209806) 11, (ClinPharm) 39, 89-90, 44-45, 96-98 |
||
Page: (NDA209803) 29, (NDA209805) 11, (NDA209806) 11, (ClinPharm) 44-45, 96-98 |
minor | yes (co-administration study) Comment: Coadministration of ertugliflozin (15 mg SD) with multiple doses of rifampicin (an inducer of UGT and CYP emzymes, 600 mg QD) decreased ertugliflozin Cmax by 15.38% and AUCinf by 38.84%. Mean terminal t1/2 was 12.3 hr for ertugliflozin administered alone compared to 9.2 hr for ertugliflozin coadministered with rifampicin., Coadministration of simvastatin (CYP3A substrate, 40 mg SD) increased Cmax of ertugliflozin (15 mg SD) by 5.16% and AUCinf by 2.40%. There are no meaningful difference in the PK of ertugliflozin when it is administered with simvastatin, as compared to single dose of ertugliflozin alone. Page: (NDA209803) 29, (NDA209805) 11, (NDA209806) 11, (ClinPharm) 44-45, 96-98 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (IND106447) 21, (NDA209803) 10, 29, 206, 207, 210 (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (IND106447) 21, (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (NDA209803) 11, 29, 206, 207,210, (NDA209805) 44, (NDA209806) 44 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=188 Page: (NDA209803) 29 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000ClinPharmR.pdf#page=43 Page: (NDA209803) 29, (ClinPharm) 42-43, 94-95 |
no | no (co-administration study) Comment: Coadministration of glimepiride (1 mg SD) decreased Cmax of ertugliflozin (15 mg SD) by 1.80% and increased AUCinf by 2.11%. There are no meaningful difference in the PK of ertugliflozin when it is administered with glimepiride, as compared to single dose of ertugliflozin alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000ClinPharmR.pdf#page=43 Page: (NDA209803) 29, (ClinPharm) 42-43, 94-95 |
||
Page: (IND106447) 21, (NDA209803) 11, 29, 206, 207,210, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 40-41, 91-92 |
no | no (co-administration study) Comment: Coadministration of metformin (OCT2 substrate, 1000 mg SD) decreased Cmax of ertugliflozin (15 mg SD) by 2.86% and increased AUCinf by 0.34%. There are no meaningful difference in the PK of ertugliflozin when it is administered with metformin, as compared to single dose of ertugliflozin alone. Page: (IND106447) 21, (NDA209803) 11, 29, 206, 207,210, (NDA209805) 44, (NDA209806) 44, (ClinPharm) 40-41, 91-92 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=45 Page: (NDA209803) 10, 29, 206, 207,120, (NDA209803) 10, (NDA209805) 44, (NDA209806) 44 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=15 Page: (IND106447) 27, (NDA209803) 29, 32, 206, 207, 210, (NDA209805) 14, 44, (NDA209806) 14, 44 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=13 Page: (IND106447) 4, 21, 22-23, (NDA209803) 22, (NDA209805) 12, (NDA209806) 12 |
||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209803,209805,209806Orig1s000PharmR.pdf#page=13 Page: (IND106447) 4, 21, (NDA209803) 22, (NDA209805) 12, (NDA209806) 12 |
PubMed
Title | Date | PubMed |
---|---|---|
From victim to ally: the kidney as an emerging target for the treatment of diabetes mellitus. | 2009 Mar |
|
Sodium glucose cotransporter 2 inhibitors as a new treatment for diabetes mellitus. | 2010 Jan |
|
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. | 2011 Apr 28 |
|
Phase III, efficacy and safety study of ertugliflozin monotherapy in people with type 2 diabetes mellitus inadequately controlled with diet and exercise alone. | 2017 May |
|
Comparative pharmacokinetics of three SGLT-2 inhibitors sergliflozin, remogliflozin and ertugliflozin: an overview. | 2017 Nov |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25754396
Once-daily ertugliflozin (1, 5, 10 or 25 mg) for the 12-week treatment period.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21690265
Ertugliflozin (PF-04971729), at a concentration range of 1.4 to 1000 μM, was evaluated as an inhibitor of the hOCT2 transporter. The calculated IC50 for inhibition of hOCT2-mediated uptake of [14C]metformin by PF-04971729 was 917 uM. Under these experimental conditions, the positive control quinidine (1 mM) inhibited >80% [14C]metformin uptake mediated by hOCT2.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:41:01 GMT 2023
by
admin
on
Sat Dec 16 11:41:01 GMT 2023
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Record UNII |
MLU731K321
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Record Status |
Validated (UNII)
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Record Version |
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1210344-83-4
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1992674
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MLU731K321
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DBSALT002616
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57339449
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100000170090
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