U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C26H26F3N3O3
Molecular Weight 485.4991
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SONIDEGIB

SMILES

C[C@@]1([H])CN(C[C@@]([H])(C)O1)c2ccc(cn2)N=C(c3cccc(c3C)-c4ccc(cc4)OC(F)(F)F)O

InChI

InChIKey=VZZJRYRQSPEMTK-CALCHBBNSA-N
InChI=1S/C26H26F3N3O3/c1-16-14-32(15-17(2)34-16)24-12-9-20(13-30-24)31-25(33)23-6-4-5-22(18(23)3)19-7-10-21(11-8-19)35-26(27,28)29/h4-13,16-17H,14-15H2,1-3H3,(H,31,33)/t16-,17+

HIDE SMILES / InChI

Molecular Formula C26H26F3N3O3
Molecular Weight 485.4991
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB09143

Sonidegib, also known as LDE225 and marketed as Odomzo, is a Hedgehog signaling pathway inhibitor (via smoothened antagonism) developed as an anticancer agent by Novartis. It was approved by the FDA for treating basal cell carcinoma in July 2015 and is awaiting approval in the EU. The hedgehog pathway is involved in many human cancers. Sonidegib effectively inhibits the regulator called smoothened (Smo), preventing the hedgehog pathway from functioning. As a result, tumours that depend on the hedgehog pathway are unable to grow. Sonidegib is approved for use in the US and EU for treatment of adults with locally advanced basal cell carcinoma (BCC) that has recurred post surgery or radiation therapy. It is also approved for adult patients with BCC who are not eligible for surgery or radiation therapy.

CNS Activity

Curator's Comment:: Sonidegib crossed the blood:brain barrier.

Originator

Curator's Comment:: # Novartis

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: Q99835
Gene ID: 6608.0
Gene Symbol: SMO
Target Organism: Homo sapiens (Human)
2.5 nM [IC50]
2.5 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ODOMZO

Approved Use

ODOMZO is a hedgehog pathway inhibitor indicated for the treatment of adult patients with locally advanced basal cell carcinoma (BCC) that has recurred following surgery or radiation therapy, or those who are not candidates for surgery or radiation therapy.

Launch Date

1.43760962E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1030 ng/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SONIDEGIB unknown
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
22 μg × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SONIDEGIB unknown
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
SONIDEGIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 3000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3000 mg, 1 times / day
Sources:
unhealthy
n = 10
Other AEs: Creatine kinase increased, Rhabdomyolysis...
Other AEs:
Creatine kinase increased (grade 3-4, 1 patient)
Rhabdomyolysis (3 patients)
Sources:
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
DLT: Creatine kinase increased...
Disc. AE: Muscle spasms, Alopecia...
Dose limiting toxicities:
Creatine kinase increased (2%)
AEs leading to
discontinuation/dose reduction:
Muscle spasms (9%)
Alopecia (6%)
Dysgeusia (5%)
Weight decreased (5%)
Fatigue (2%)
Asthenia (1%)
Nausea (4%)
Decreased appetite (5%)
Arthralgia (1%)
Dysphagia (1%)
General physical health deterioration (1%)
Ageusia (2%)
Dehydration (2%)
Sources: Page: 104
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 105
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 105
Disc. AE: Anemia, Constipation...
AEs leading to
discontinuation/dose reduction:
Anemia (1%)
Constipation (1%)
Hypertension (1%)
Hypogeusia (1%)
Sources: Page: 105
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Disc. AE: Diarrhea, Gastroenteritis viral...
AEs leading to
discontinuation/dose reduction:
Diarrhea (5%)
Gastroenteritis viral (1%)
Rhabdomyolysis (1%)
Alanine aminotransferase increased (2%)
Aspartate aminotransferase increased (2%)
Dizziness (1%)
Myalgia (3%)
Muscular weakness (1%)
Blood uric acid increased (1%)
Vomiting (7%)
Dyspnea (1%)
Myoglobin blood increased (1%)
Hypogeusia (1%)
Amylase increased (1%)
Malaise (1%)
Sources: Page: 106
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Disc. AE: Amylase increased...
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Disc. AE: Alanine aminotransferase increased, Aspartate aminotransferase increased...
AEs leading to
discontinuation/dose reduction:
Alanine aminotransferase increased (grade 3-4, 4%)
Aspartate aminotransferase increased (all grades, 19%)
Asthenia (4%)
Sources:
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Disc. AE: Muscle spasms, Myalgia...
Other AEs: Muscle spasms, Musculoskeletal pain...
AEs leading to
discontinuation/dose reduction:
Muscle spasms (grade 3, 3%)
Myalgia (all grades, 19%)
Alopecia (all grades, 53%)
Diarrhea (grade 3, 1%)
Weight decreased (grade 3, 3%)
Decreased appetite (grade 3, 1%)
Other AEs:
Muscle spasms (all grades, 54%)
Musculoskeletal pain (all grades, 32%)
Musculoskeletal pain (grade 3, 1%)
Pruritus (all grades, 10%)
Headache (all grades, 15%)
Headache (grade 3, 1%)
Fatigue (all grades, 41%)
Pain (all grades, 14%)
Pain (grade 3, 1%)
Nausea (all grades, 39%)
Diarrhea (all grades, 32%)
Abdominal pain (all grades, 18%)
Vomiting (all grades, 11%)
Weight decreased (all grades, 30%)
Decreased appetite (all grades, 23%)
Increased serum creatinine (all grades, 92%)
Creatine kinase increased (all grades, 61%)
Hyperglycemia (all grades, 51%)
Hyperglycemia (grade 3-4, 4%)
Lipase increased (all grades, 43%)
Alanine aminotransferase increased (all grades, 19%)
Aspartate aminotransferase increased (grade 3-4, 4%)
Amylase increased (all grades, 16%)
Anemia (all grades, 32%)
Lymphopenia (all grades, 28%)
Lymphopenia (grade 3-4, 3%)
Sources:
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Disc. AE: Dysgeusia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Dysgeusia (all grades, 46%)
Fatigue (grade 3, 4%)
Nausea (grade 3, 1%)
Vomiting (grade 3, 1%)
Creatine kinase increased (grade 3-4, 8%)
Lipase increased (grade 3-4, 13%)
Sources:
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Disc. AE: Arthralgia, Dysphagia...
AEs leading to
discontinuation/dose reduction:
Arthralgia (1 patient)
Dysphagia (1 patient)
General physical health deterioration (1 patient)
Abdominal pain upper (1 patient)
Agitation (1 patient)
Depression (1 patient)
Dry mouth (1 patient)
Lumbar vertebral fracture (1 patient)
Sources: Page: 104
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 106
Disc. AE: Rhabdomyolysis, Dizziness...
AEs leading to
discontinuation/dose reduction:
Rhabdomyolysis (1%)
Dizziness (1%)
Pneumonia (1%)
Muscular weakness (1%)
Sources: Page: 106
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Disc. AE: Blood uric acid increased, Angina pectoris...
AEs leading to
discontinuation/dose reduction:
Blood uric acid increased (1%)
Angina pectoris (1%)
Anorectal infection (1%)
Back pain (1%)
Bile duct stone (1%)
Cough (1%)
Disturbance in attention (1%)
Femoral neck fracture (1%)
Gastric ulcer (1%)
Influenza (1%)
Sleep disorder (1%)
Spinal compression fracture (1%)
Upper respiratory tract infection (1%)
Sources: Page: 107
AEs

AEs

AESignificanceDosePopulation
Rhabdomyolysis 3 patients
3000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 3000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3000 mg, 1 times / day
Sources:
unhealthy
n = 10
Creatine kinase increased grade 3-4, 1 patient
3000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 3000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3000 mg, 1 times / day
Sources:
unhealthy
n = 10
Arthralgia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Asthenia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Dysphagia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
General physical health deterioration 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Creatine kinase increased 2%
DLT, Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Ageusia 2%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Dehydration 2%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Fatigue 2%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Nausea 4%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Decreased appetite 5%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Dysgeusia 5%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Weight decreased 5%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Alopecia 6%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Muscle spasms 9%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 104
Anemia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 105
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 105
Constipation 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 105
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 105
Hypertension 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 105
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 105
Hypogeusia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 105
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 105
Amylase increased 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Blood uric acid increased 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Dizziness 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Dyspnea 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Gastroenteritis viral 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Hypogeusia 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Malaise 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Muscular weakness 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Myoglobin blood increased 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Rhabdomyolysis 1%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Alanine aminotransferase increased 2%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Aspartate aminotransferase increased 2%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Myalgia 3%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Diarrhea 5%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Vomiting 7%
Disc. AE
800 mg 1 times / day steady, oral
MTD
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 150
Health Status: unhealthy
Population Size: 150
Sources: Page: 106
Amylase increased grade 3-4, 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Asthenia 4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Aspartate aminotransferase increased all grades, 19%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Alanine aminotransferase increased grade 3-4, 4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Pruritus all grades, 10%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Vomiting all grades, 11%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Pain all grades, 14%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Headache all grades, 15%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Amylase increased all grades, 16%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Abdominal pain all grades, 18%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Alanine aminotransferase increased all grades, 19%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Myalgia all grades, 19%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Decreased appetite all grades, 23%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Lymphopenia all grades, 28%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Weight decreased all grades, 30%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Anemia all grades, 32%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Diarrhea all grades, 32%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Musculoskeletal pain all grades, 32%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Nausea all grades, 39%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Fatigue all grades, 41%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Lipase increased all grades, 43%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Hyperglycemia all grades, 51%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Alopecia all grades, 53%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Muscle spasms all grades, 54%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Creatine kinase increased all grades, 61%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Increased serum creatinine all grades, 92%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Headache grade 3, 1%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Musculoskeletal pain grade 3, 1%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Pain grade 3, 1%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Decreased appetite grade 3, 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Diarrhea grade 3, 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Muscle spasms grade 3, 3%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Weight decreased grade 3, 3%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Lymphopenia grade 3-4, 3%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Aspartate aminotransferase increased grade 3-4, 4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Hyperglycemia grade 3-4, 4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources:
Dysgeusia all grades, 46%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Nausea grade 3, 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Vomiting grade 3, 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Fatigue grade 3, 4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Lipase increased grade 3-4, 13%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Creatine kinase increased grade 3-4, 8%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
unhealthy
n = 79
Abdominal pain upper 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Agitation 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Arthralgia 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Depression 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Dry mouth 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Dysphagia 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
General physical health deterioration 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Lumbar vertebral fracture 1 patient
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 104
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 104
Dizziness 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 106
Muscular weakness 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 106
Pneumonia 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 106
Rhabdomyolysis 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 106
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 106
Angina pectoris 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Anorectal infection 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Back pain 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Bile duct stone 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Blood uric acid increased 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Cough 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Disturbance in attention 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Femoral neck fracture 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Gastric ulcer 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Influenza 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Sleep disorder 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Spinal compression fracture 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Upper respiratory tract infection 1%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources: Page: 107
unhealthy
n = 79
Health Status: unhealthy
Condition: locally advanced BCC
Population Size: 79
Sources: Page: 107
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 1.5 uM]
yes [Ki 0.045 uM]
unknown (co-administration study)
Comment: study to assess the effects of sonidegib on the PK of a CYP2B6 and a CYP2C9 probe substrate is ongoing
Page: -
yes [Ki 1.7 uM]
unknown (co-administration study)
Comment: study to assess the effects of sonidegib on the PK of a CYP2B6 and a CYP2C9 probe substrate is ongoing
Page: -
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Sonidegib is metabolized by CYP3A4 to several inactive metabolites. Ketoconazole increased sonidegib AUC0-10d by 2.2-fold and rifampicin decreased sonidegib AUC0-10d by 72% following a single 800 mg dose in healthy subjects.
Page: -
no
no
no
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist.
2010 Jun 10
Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.
2012 Nov 15
Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.
2014 Jul
Patents

Sample Use Guides

Recommended dose: 200 mg orally once daily taken on an empty stomach, at least 1 hour before or 2 hours after a meal.
Route of Administration: Oral
Sonidegib inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively.
Substance Class Chemical
Created
by admin
on Sat Jun 26 01:09:18 UTC 2021
Edited
by admin
on Sat Jun 26 01:09:18 UTC 2021
Record UNII
0RLU3VTK5M
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SONIDEGIB
DASH   INN   USAN   WHO-DD  
INN   USAN  
Official Name English
(1,1'-BIPHENYL)-3-CARBOXAMIDE, N-(6-((2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL)-3-PYRIDINYL)-2-METHYL-4'-(TRIFLUOROMETHOXY)-, REL-
Common Name English
LDE 225
Code English
SONIDEGIB [INN]
Common Name English
SONIDEGIB [WHO-DD]
Common Name English
NVP-LDE225
Code English
SONIDEGIB [USAN]
Common Name English
NVP-LDE 225
Code English
N-(6-((2R,6S)-2,6-DIMETHYLMORPHOLIN-4-YL)PYRIDIN-3-YL)-2-METHYL-4'-(TRIFLUOROMETHOXY)BIPHENYL-3-CARBOXAMIDE
Systematic Name English
N-(6-((CIS-2,6-DIMETHYLMORPHOLIN-4-YL)-3-PYRIDYL)-2-METHYL-3-(4-(TRIFLUOROMETHOXY)PHENYL)BENZAMIDE
Common Name English
LDE-225
Code English
LDE225
Code English
NVP-LDE-225
Code English
ERISMODEGIB
Common Name English
SONIDEGIB [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C2189
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
WHO-ATC L01XX48
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
FDA ORPHAN DRUG 468814
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
NDF-RT N0000184149
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
Code System Code Type Description
LACTMED
Sonidegib
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
RXCUI
1659191
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY RxNorm
IUPHAR
8199
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
NDF-RT
N0000184148
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY Smoothened Receptor Antagonists [MoA]
ChEMBL
CHEMBL2105737
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
DRUG BANK
DB09143
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
CAS
956697-53-3
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
DRUG CENTRAL
5008
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
WIKIPEDIA
SONIDEGIB
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
EU-Orphan Drug
EU/3/09/697(WITHDRAWN)
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY Treatment of naevoid basal-cell carcinoma syndrome (Gorlin syndrome) 24/11/2009 Withdrawn
FDA UNII
0RLU3VTK5M
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
MERCK INDEX
M11843
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
NCI_THESAURUS
C82385
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
PUBCHEM
24775005
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
INN
9394
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
EVMPD
SUB123432
Created by admin on Sat Jun 26 01:09:19 UTC 2021 , Edited by admin on Sat Jun 26 01:09:19 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> NON-INDUCER
compared to positive controls
TARGET -> INHIBITOR
IC50
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> NON-INDUCER
compared to positive controls
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> INHIBITOR
Ki
METABOLIC ENZYME -> SUBSTRATE
metabolism by CYP3A4 (at least 29% of its overall metabolism); Ketoconazole(CYP 3A4 inhibition) increased sonidegib exposure 2.2-fold;Rifampin (CYP 3A4 induction) reduced exposure by 72%
METABOLIC ENZYME -> NON-INHIBITOR
No time dependent inhibition upto 50 micromolar
METABOLIC ENZYME -> INHIBITOR
Ki
Related Record Type Details
METABOLITE ACTIVE -> PARENT
LNC-119 AND LMT-326 ACCOUNTED FOR 14% OF THE AUC
PLASMA
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE ACTIVE -> PARENT
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC