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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H25ClO7
Molecular Weight 436.8835
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ERTUGLIFLOZIN

SMILES

CCOc1ccc(cc1)Cc2cc(ccc2Cl)[C@]34[C@@]([H])([C@]([H])([C@@]([H])([C@](CO)(CO3)O4)O)O)O

InChI

InChIKey=MCIACXAZCBVDEE-CUUWFGFTSA-N
InChI=1S/C22H25ClO7/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/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3/t18-,19-,20+,21-,22-/m0/s1

HIDE SMILES / InChI

Molecular Formula C22H25ClO7
Molecular Weight 436.8835
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

Curator's Comment:: # Pfizer, Inc.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.877000000000000002 nM [IC50]
1960 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ERTUGLIFLOZIN
Primary
STEGLATRO

Approved Use

STEGLATRO™ is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Launch Date

1513555200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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:
unhealthy, > 65 years
Disc. AE: Hyperglycaemia, Glomerular filtration rate decreased...
AEs leading to
discontinuation/dose reduction:
Hyperglycaemia (0.5%)
Glomerular 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%)
Sources:
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Disc. AE: Hyperglycaemia, Glomerular filtration rate decreased...
AEs leading to
discontinuation/dose reduction:
Hyperglycaemia (0.3%)
Glomerular 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%)
Sources:
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:
unhealthy, adult
Other AEs: Acute myocardial infarction, Haemorrhagic stroke...
Other AEs:
Acute myocardial infarction (grade 5, 0.18%)
Haemorrhagic stroke (grade 5, 0.06%)
Ischaemic stroke (grade 5, 0.06%)
Septic shock (grade 5, 0.06%)
Plasma cell myeloma (grade 5, 0.06%)
Sources:
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Other AEs: Acute myocardial infarction, Cardiac death...
Other AEs:
Acute myocardial infarction (grade 5, 0.06%)
Cardiac 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%)
Sources:
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
Health Status: healthy
Sources:
300 mg single, oral
Highest studied dose
Dose: 300 mg
Route: oral
Route: single
Dose: 300 mg
Sources:
healthy
Health Status: healthy
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
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:
unhealthy, > 65 years
Abdominal pain upper 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Acute kidney injury 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Acute myocardial infarction 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Acute pancreatitis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Adenocarcinoma gastric 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Alanine aminotransferase increased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Aspartate aminotransferase increased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Asthenia 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Blood creatinine increased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Blood glucose increased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Breast cancer 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Cerebral infarction 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Cerebrovascular accident 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Coronary artery disease 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Diabetic foot 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Diabetic neuropathy 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Diarrhoea 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Dyslipidaemia 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Dysuria 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Face injury 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Facial paralysis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Fungal skin infection 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Genital candidiasis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Genital infection 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Glomerular filtration rate decreased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Head discomfort 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Hepatocellular injury 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Humerus fracture 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Hunger 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Hyperchlorhydria 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Hypoglycaemia 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Insomnia 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Musculoskeletal pain 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Myocardial infarction 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Nausea 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Nephropathy 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Non-cardiac chest pain 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Obesity 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Oral candidiasis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Osteomyelitis acute 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Pain in extremity 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Pollakiuria 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Polyuria 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Pruritus genital 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Pyelonephritis acute 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Pyelonephritis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Rash 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Rheumatoid arthritis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Thirst 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Urinary retention 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Urinary tract infection 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Urogenital infection fungal 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Vaginal infection 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Vulvovaginal candidiasis 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Vulvovaginal pruritus 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Weight decreased 0.1%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Dizziness 0.2%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Vulvovaginal mycotic infection 0.2%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Balanoposthitis 0.3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
Hyperglycaemia 0.3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, > 65 years
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:
unhealthy, adult
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:
unhealthy, adult
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:
unhealthy, adult
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:
unhealthy, adult
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:
unhealthy, adult
Acute myocardial infarction grade 5, 0.06%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Chronic obstructive pulmonary disease grade 5, 0.06%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Depression grade 5, 0.06%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Multiple organ dysfunction syndrome grade 5, 0.06%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Pneumonia grade 5, 0.06%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Cardiac death grade 5, 0.17%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
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
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
no [IC50 >30 uM]
Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [IC50 >30 uM]
Page: (IND106447) 21, (NDA209803) 10, 27, 206, 207, (NDA209805) 11, 44, (NDA209806) 11, 44
no [IC50 >30 uM]
Page: (IND106447) 21, (NDA209803) 10, 27, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [IC50 >30 uM]
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
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
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
Page: (NDA209803) 11, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [Ki >250 uM]
Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [Ki >50 uM]
Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [Ki >50 uM]
Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no [Ki >50 uM]
Page: (IND122329) 15, (IND106447) 21, (NDA209803) 27, 29, 206, 207, 210(NDA209803) 10, (NDA209805) 44, (NDA209806) 44
no
Page: (NDA209803) 10, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
no
Page: (IND106447) 21, (NDA209803) 27, 29, 206, 207, 210, (NDA209803) 10, (NDA209805) 44, (NDA209806) 44
no
weak [IC50 140.7 uM]
Page: (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44
weak [IC50 176 uM]
weak [IC50 35.4 uM]
Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
weak [IC50 39 uM]
Page: (NDA209803) 10, 28, 29, 206, 207, (NDA209805) 44, (NDA209806) 44
weak [IC50 45 uM]
weak [IC50 53 uM]
Page: (IND106447) 21, (NDA209803) 11, 28, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44
weak [IC50 70 uM]
weak [Inhibition 100 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
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.
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.
Page: (NDA209803) 10, 29, (NDA209805) 11, 43, (NDA209806) 11, 43
minor
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
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
no
no
no
no
Page: (IND106447) 21, (NDA209803) 10, 29, 206, 207, 210 (NDA209805) 44, (NDA209806) 44
no
Page: (IND106447) 21, (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44
no
Page: (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44
no
Page: (NDA209803) 11, 29, 206, 207, 210, (NDA209805) 44, (NDA209806) 44
no
Page: (NDA209803) 11, 29, 206, 207,210, (NDA209805) 44, (NDA209806) 44
no
no
no
no
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.
Page: (NDA209803) 29, (ClinPharm) 42-43, 94-95
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
Page: (NDA209803) 10, 29, 206, 207,120, (NDA209803) 10, (NDA209805) 44, (NDA209806) 44
yes
Page: (IND106447) 27, (NDA209803) 29, 32, 206, 207, 210, (NDA209805) 14, 44, (NDA209806) 14, 44
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Page: (IND106447) 4, 21, 22-23, (NDA209803) 22, (NDA209805) 12, (NDA209806) 12
Page: (IND106447) 4, 21, (NDA209803) 22, (NDA209805) 12, (NDA209806) 12
PubMed

PubMed

TitleDatePubMed
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
Patents

Sample Use Guides

Once-daily ertugliflozin (1, 5, 10 or 25 mg) for the 12-week treatment period.
Route of Administration: Oral
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 Sat Jun 26 08:23:42 UTC 2021
Edited
by admin
on Sat Jun 26 08:23:42 UTC 2021
Record UNII
6C282481IP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ERTUGLIFLOZIN
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
ERTUGLIFLOZIN [WHO-DD]
Common Name English
PF04971729
Code English
(1S,2S,3S,4R,5S)-5-(4-CHLORO-3-((4-ETHOXYPHENYL)METHYL)PHENYL)- 1-(HYDROXYMETHYL)-6,8-DIOXABICYCLO(3.2.1)OCTANE-2,3,4-TRIOL
Systematic Name English
ERTUGLIFLOZIN COMPONENT OF STELUJAN
Brand Name English
STEGLATRO
Brand Name English
ERTUGLIFLOZIN [MI]
Common Name English
.BETA.-L-IDOPYRANOSE, 1,6-ANHYDRO-1-C-(4-CHLORO-3-((4-ETHOXYPHENYL)METHYL)PHENYL)-5-C-(HYDROXYMETHYL)-
Common Name English
PF-04971729
Common Name English
ERTUGLIFLOZIN [ORANGE BOOK]
Common Name English
ERTUGLIFLOZIN COMPONENT OF SEGLUROMET
Brand Name English
ERTUGLIFLOZIN [INN]
Common Name English
STELUJAN COMPONENT ERTUGLIFLOZIN
Brand Name English
SEGLUROMET COMPONENT ERTUGLIFLOZIN
Brand Name English
ERTUGLIFLOZIN [USAN]
Common Name English
PF-04971729-00
Code English
Classification Tree Code System Code
WHO-ATC A10BD24
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
WHO-ATC A10BK04
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C166925
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
EPA CompTox
1210344-57-2
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
DRUG CENTRAL
5270
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
CAS
1210344-57-2
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
DRUG BANK
DB11827
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
PUBCHEM
44814423
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
FDA UNII
6C282481IP
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
MERCK INDEX
M12059
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
ChEMBL
CHEMBL1770248
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
EVMPD
SUB182716
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
LACTMED
Ertugliflozin
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
INN
9460
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
RXCUI
1992672
Created by admin on Sat Jun 26 08:23:42 UTC 2021 , Edited by admin on Sat Jun 26 08:23:42 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
CHO CELLS STABLY EXPRESSING HUMAN SGLT2, MEASURING THE SODIUM DEPENDENT UPTAKE OF 14C-LABELED METHYL-ALPHA-D-GLUCOPYRANOSIDE (AMG) (N=10)
INHIBITOR
IC50
BINDER->LIGAND
BINDING
TRANSPORTER -> SUBSTRATE
CUMULATIVE EXCRETION
FECAL
TRANSPORTER -> INHIBITOR
IC50
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
CUMULATIVE EXCRETION
URINE
METABOLIC ENZYME -> INHIBITOR
IC50
EXCRETED UNCHANGED
FECAL
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC DOSE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC
DOSE
PHARMACOKINETIC
Tmax PHARMACOKINETIC ROUTE OF ADMINISTRATION
PHARMACOKINETIC
DOSE
PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC ROUTE OF ADMINISTRATION