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

Details

Stereochemistry ABSOLUTE
Molecular Formula C30H30F2N6O3
Molecular Weight 560.5944
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0
Stereo Comments AXIAL, R

SHOW SMILES / InChI
Structure of SOTORASIB

SMILES

CC(C)C1=C(N2C(=O)N=C(N3CCN(C[C@@H]3C)C(=O)C=C)C4=CC(F)=C(N=C24)C5=C(O)C=CC=C5F)C(C)=CC=N1

InChI

InChIKey=NXQKSXLFSAEQCZ-SFHVURJKSA-N
InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1

HIDE SMILES / InChI

Molecular Formula C30H30F2N6O3
Molecular Weight 560.5944
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Sotorasib (LUMAKRAS™) is a RAS GTPase family inhibitor being developed by Amgen for the treatment of solid tumours with KRAS mutations, including non-small cell lung cancer (NSCLC) and colorectal cancer. Sotorasib is an inhibitor of KRASG12C, a tumor-restricted, mutant-oncogenic form of the RAS GTPase, KRAS. Sotorasib forms an irreversible, covalent bond with the unique cysteine of KRASG12C, locking the protein in an inactive state that prevents downstream signaling without affecting wild-type KRAS. Sotorasib blocked KRAS signaling, inhibited cell growth, and promoted apoptosis only in KRAS G12C tumor cell lines. Sotorasib inhibited KRASG12C in vitro and in vivo with minimal detectable off-target activity. In May 2021, sotorasib was granted accelerated approval by the US FDA for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic NSCLC, as determined by an FDA-approved test, who have received at least one prior systemic therapy.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LUMAKRAS

Approved Use

LUMAKRAS is an inhibitor of the RAS GTPase family indicated for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy.

Launch Date

2021
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6.44 μg/mL
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
6.31 μg/mL
360 mg 1 times / day steady-state, oral
dose: 360 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5.45 μg/mL
720 mg 1 times / day steady-state, oral
dose: 720 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5.39 μg/mL
960 mg 1 times / day steady-state, oral
dose: 960 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
6690 ng/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
7880 ng/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
8320 ng/mL
960 mg 1 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
7180 ng/mL
960 mg 1 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
31.7 μg × h/mL
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
38.9 μg × h/mL
360 mg 1 times / day steady-state, oral
dose: 360 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
42.1 μg × h/mL
720 mg 1 times / day steady-state, oral
dose: 720 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
32.4 μg × h/mL
960 mg 1 times / day steady-state, oral
dose: 960 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
28700 ng × h/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
31500 ng × h/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
81500 ng × h/mL
960 mg 1 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
43900 ng × h/mL
960 mg 1 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.13 h
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
5.53 h
360 mg 1 times / day steady-state, oral
dose: 360 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4.75 h
720 mg 1 times / day steady-state, oral
dose: 720 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5.07 h
960 mg 1 times / day steady-state, oral
dose: 960 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOTORASIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound
Doses

Doses

DosePopulationAdverse events​
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Disc. AE: Vomiting, Gastric ulcer...
Other AEs: Pneumonia...
AEs leading to
discontinuation/dose reduction:
Vomiting (1 patient)
Gastric ulcer (1 patient)
Pneumonitis (2 patients)
Hepatobiliary disorders (3 patients)
Haemorrhage intracranial (1 patient)
Cardiac arrest (1 patient)
Alanine aminotransferase increased (4 patients)
Aspartate aminotransferase increased (4 patients)
Pneumothorax (2 patients)
Liver function test increased (1 patient)
Dehydration (1 patient)
Neoplasms (1 patient)
Dyspnea (1 patient)
Pneumothorax (1 patient)
Gastric ulcer (2 patients)
Other AEs:
Pneumonia (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Pneumonia 1 patient
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Cardiac arrest 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Dehydration 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Dyspnea 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Gastric ulcer 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Haemorrhage intracranial 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Liver function test increased 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Neoplasms 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pneumothorax 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Vomiting 1 patient
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Gastric ulcer 2 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pneumonitis 2 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pneumothorax 2 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Hepatobiliary disorders 3 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Alanine aminotransferase increased 4 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Aspartate aminotransferase increased 4 patients
Disc. AE
960 mg 1 times / day steady, oral
Highest studied dose
Dose: 960 mg, 1 times / day
Route: oral
Route: steady
Dose: 960 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes [IC50 0.44 uM]
no (co-administration study)
Comment: No significant effect on metformin AUCinf and Cmax (0.985-fold and 0.996-fold)
Page: 57.0
yes [IC50 120 uM]
yes [IC50 2.39 uM]
no (co-administration study)
Comment: No significant effect on metformin AUCinf and Cmax (0.985-fold and 0.996-fold)
Page: 57.0
yes [IC50 60.2 uM]
yes (co-administration study)
Comment: Increased digoxin AUCinf and Cmax by 1.214-fold and 1.914-fold
Page: 57 | 91
yes [Ki 18.1 uM]
yes
yes
yes
yes
yes (co-administration study)
Comment: Decreased midazolam AUCinf and Cmax by 0.47-fold and 0.52-fold
Page: 91.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
weak (co-administration study)
Comment: Rifampicin decreased AUCinf and Cmax by 0.766-fold and 0.840-fold
Page: 91 | 97
weak (co-administration study)
Comment: Rifampicin decreased AUCinf and Cmax by 0.766-fold and 0.840-fold
Page: 91 | 97
minor
minor
yes (co-administration study)
Comment: Rifampicin decreased AUCinf and Cmax by 0.487-fold and 0.647-fold
Page: 57 | 91
no
no
no (co-administration study)
Comment: No significant effect on sotorasib AUCinf and Cmax (0.910-fold and 0.812-fold)
Page: 91.0
no
no (co-administration study)
Comment: No significant effect on sotorasib AUCinf and Cmax (0.910-fold and 0.812-fold)
Page: 91.0
yes
weak (co-administration study)
Comment: Itraconazole increased AUCinf by 1.261-fold but did not affect on Cmax (1.040-fold)
Page: 57.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Sotorasib for previously treated colorectal cancers with KRASG12C mutation (CodeBreaK100): a prespecified analysis of a single-arm, phase 2 trial.
2022-01
Sotorasib: First Approval.
2021-09
Sotorasib for Lung Cancers with KRAS p.G12C Mutation.
2021-06-24
KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors.
2020-09-24
Patents

Sample Use Guides

In Vivo Use Guide
Sources: Recommended dosage: 960 mg orally once daily
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214665s000lbl.pdf
Route of Administration: Oral
Sotorasib inhibited the SOS1- catalyzed nucleotide exchange of KRASG12C (IC50 = 92.6 nM or ~51.9 ng/mL) but not wild-type (WT) KRAS (IC50 >250 uM).
Substance Class Chemical
Created
by admin
on Wed Apr 02 00:10:03 GMT 2025
Edited
by admin
on Wed Apr 02 00:10:03 GMT 2025
Record UNII
2B2VM6UC8G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SOTORASIB
USAN   INN  
Official Name English
6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-(1M)-1-(4-METHYL-2-(PROPAN-2-YL)PYRIDIN-3-YL)-4-((2S)-2-METHYL-4-(PROP-2-ENOYL)PIPERAZIN-1-YL)PYRIDO(2,3-D)PYRIMIDIN-2(1H)-ONE
Preferred Name English
SOTORASIB [JAN]
Common Name English
SOTORASIB [ORANGE BOOK]
Common Name English
sotorasib [INN]
Common Name English
KRAS MUTANT-TARGETING AMG 510
Common Name English
Sotorasib [WHO-DD]
Common Name English
PYRIDO(2,3-D)PYRIMIDIN-2(1H)-ONE, 6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-(4-METHYL-2-(1-METHYLETHYL)-3-PYRIDINYL)-4-((2S)-2-METHYL-4-(1-OXO-2-PROPEN-1-YL)-1-PIPERAZINYL)-
Systematic Name English
PYRIDO(2,3-D)PYRIMIDIN-2(1H)-ONE, 6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-(4-METHYL-2-(1-METHYLETHYL)-3-PYRIDINYL)-4-((2S)-2-METHYL-4-(1-OXO-2-PROPEN-1-YL)-1-PIPERAZINYL)-, (1R)-
Systematic Name English
AMG-510
Code English
LUMAKRAS
Brand Name English
AMG510
Code English
(1RA)-6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-4-((2S)-2-METHYL-4-(1-OXOPROP-2-EN-1-YL)PIPERAZIN-1-YL)-1-(4-METHYL-2-(PROPAN-2-YL)PYRIDIN-3-YL)PYRIDO(2,3-D)PYRIMIDIN-2(1H)-ONE
Systematic Name English
(1M)-6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-(4-METHYL-2-(PROPAN-2-YL)PYRIDIN-3-YL)-4-((2S)-2-METHYL-4-(PROP-2-ENOYL)PIPERAZIN-1-YL)PYRIDO(2,3-D)PYRIMIDIN-2(1H)-ONE
Systematic Name English
SOTORASIB [USAN]
Common Name English
KRAS G12C INHIBITOR 9
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 654918
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
FDA ORPHAN DRUG 653818
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
Code System Code Type Description
FDA UNII
2B2VM6UC8G
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
PUBCHEM
137278711
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
CAS
2252403-56-6
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
NON-SPECIFIC STEREOCHEMISTRY
DAILYMED
2B2VM6UC8G
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
USAN
HI-164
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
WIKIPEDIA
Sotorasib
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
CAS
2296729-00-3
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
DRUG BANK
DB15569
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
INN
11370
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
SMS_ID
100000183068
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
NCI_THESAURUS
C154287
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
EPA CompTox
DTXSID001099260
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
RXCUI
2550714
Created by admin on Wed Apr 02 00:10:03 GMT 2025 , Edited by admin on Wed Apr 02 00:10:03 GMT 2025
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
IC50
PROTEIN ADDUCT FORMATION
OFF-TARGET->INHIBITOR
Weak Inhibitor
TARGET -> INHIBITOR
Selective for G12C mutant. Approved to target KRAS G12C mutations in the second-line setting.
IRREVERSIBLE INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
EXCRETED UNCHANGED
FECAL
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
IC50
BINDER->LIGAND
Related Record Type Details
METABOLITE LESS ACTIVE -> PARENT
IRREVERSIBLE INHIBITOR
IC50
METABOLITE INACTIVE -> PARENT
METABOLITE INACTIVE -> PARENT
Mediated primarily by nonenzymatic glutathione conjugation
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC