Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
Ras protein inhibitors	5461	2296729-00-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sotorasib lumakras AMG510	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 mouse tumor xenograft models sotorasib-treatment led to tumor regressions and prolonged survival and was associated with anti-tumor immunity in KRAS G12C models. Molecular weight: 559.62 Formula: C31H31F2N5O3 CLOGP: 5.90 LIPINSKI: 1 HAC: 9 HDO: 1 TPSA: 98.99 ALOGS: -4.48 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sotorasib
lumakras
AMG510

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 mouse tumor xenograft models sotorasib-treatment led to tumor regressions and prolonged survival and was associated with anti-tumor immunity in KRAS G12C models.

Molecular weight: 559.62
Formula: C31H31F2N5O3
CLOGP: 5.90
LIPINSKI: 1
HAC: 9
HDO: 1
TPSA: 98.99
ALOGS: -4.48
ROTB: 3

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	EIF2AK3,PDK1,PDK2,PDK4	4
kinase-selectivity-class	BMX	1
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	14.655		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
rat-kpuu-brain	Rat brain Kpuu	0.006	%	High	1

Approvals:

Date	Agency	Company
May 28, 2021	FDA	AMGEN INC
Jan. 6, 2022	EMA	Amgen Europe BV
Jan. 20, 2022	PMDA	AMGEN K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Non-small cell lung cancer	344.62	49.70	58	1132	4323	90622934
Non-small cell lung cancer metastatic	200.50	49.70	29	1161	789	90626468
Diarrhoea	99.75	49.70	88	1102	939102	89688155
Death	94.99	49.70	64	1126	456487	90170770
Hepatotoxicity	92.18	49.70	31	1159	45811	90581446
Alanine aminotransferase increased	66.75	49.70	32	1158	118306	90508951
Aspartate aminotransferase increased	64.70	49.70	30	1160	102907	90524350
Hepatic function abnormal	61.39	49.70	23	1167	46265	90580992
Therapy partial responder	60.94	49.70	19	1171	22024	90605233
Disease progression	58.27	49.70	32	1158	156583	90470674
Hepatic cytolysis	50.79	49.70	18	1172	30898	90596359

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Non-small cell lung cancer	852.14	41.51	147	1336	4827	42615025
Non-small cell lung cancer metastatic	234.85	41.51	38	1445	805	42619047
Hepatic function abnormal	136.01	41.51	55	1428	51512	42568340
Death	85.06	41.51	92	1391	471093	42148759
Diarrhoea	77.91	41.51	87	1396	460762	42159090
Disease progression	61.67	41.51	46	1437	143610	42476242
Lung adenocarcinoma	60.06	41.51	17	1466	5322	42614530
Aspartate aminotransferase increased	50.28	41.51	32	1451	77131	42542721
Metastases to central nervous system	45.14	41.51	16	1467	10339	42609513

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Non-small cell lung cancer	852.93	43.12	145	2003	7790	110579361
Non-small cell lung cancer metastatic	275.70	43.12	43	2105	1309	110585842
Disease progression	205.64	43.12	98	2050	243936	110343215
Death	135.94	43.12	110	2038	698759	109888392
Diarrhoea	130.58	43.12	133	2015	1139372	109447779
Hepatic function abnormal	127.16	43.12	52	2096	89243	110497908
Lung adenocarcinoma	97.97	43.12	25	2123	9506	110577645
Aspartate aminotransferase increased	86.99	43.12	48	2100	159888	110427263
Hepatic cytolysis	81.48	43.12	33	2115	55020	110532131
Therapy partial responder	79.09	43.12	29	2119	37032	110550119
Alanine aminotransferase increased	75.58	43.12	46	2102	183727	110403424
Hepatotoxicity	54.67	43.12	26	2122	63374	110523777
Cholestasis	54.24	43.12	26	2122	64492	110522659
Lung neoplasm malignant	45.65	43.12	19	2129	33823	110553328

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XX73	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
MeSH PA	D000970	Antineoplastic Agents
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer	indication	254637007	DOID:3908

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	12280056	Nov. 18, 2039	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	12280056	Nov. 18, 2039	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	12280056	Nov. 18, 2039	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11236091	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11236091	May 20, 2040	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
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11827635	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11827635	May 20, 2040	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
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	12398133	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	12398133	May 20, 2040	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
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11236091	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11236091	May 20, 2040	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
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11827635	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11827635	May 20, 2040	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
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	12398133	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	12398133	May 20, 2040	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
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11236091	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11236091	May 20, 2040	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
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11827635	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11827635	May 20, 2040	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
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	12398133	May 20, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	12398133	May 20, 2040	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
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11426404	Sept. 15, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	11426404	Sept. 15, 2040	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
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11426404	Sept. 15, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	11426404	Sept. 15, 2040	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
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11426404	Sept. 15, 2040	IN COMBINATION WITH PANITUMUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	11426404	Sept. 15, 2040	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

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	Jan. 16, 2028	IN COMBINATION WITH PANITUMUMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	Jan. 16, 2028	IN COMBINATION WITH PANITUMUMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	Jan. 16, 2028	IN COMBINATION WITH PANITUMUMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	May 28, 2028	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
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	May 28, 2028	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	May 28, 2028	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
120MG	LUMAKRAS	AMGEN INC	N214665	May 28, 2021	RX	TABLET	ORAL	Jan. 16, 2032	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-AND IRINOTECAN-BASED CHEMOTHERAPY
240MG	LUMAKRAS	AMGEN INC	N214665	June 26, 2024	RX	TABLET	ORAL	Jan. 16, 2032	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-AND IRINOTECAN-BASED CHEMOTHERAPY
320MG	LUMAKRAS	AMGEN INC	N214665	Jan. 20, 2023	RX	TABLET	ORAL	Jan. 16, 2032	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED METASTATIC COLORECTAL CANCER (MCRC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED PRIOR FLUOROPYRIMIDINE-, OXALIPLATIN-AND IRINOTECAN-BASED CHEMOTHERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GTPase KRas	Enzyme	P01116	RASK_HUMAN	INHIBITOR	IC50	7.03		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
D12055	KEGG_DRUG
2B2VM6UC8G	UNII
C5418250	UMLSCUI
CHEBI:178199	CHEBI
CHEMBL4535757	ChEMBL_ID
137278711	PUBCHEM_CID
DB15569	DRUGBANK_ID
11370	INN_ID
C000706028	MESH_SUPPLEMENTAL_RECORD_UI
10678	IUPHAR_LIGAND_ID
1162482008	SNOMEDCT_US
1162509004	SNOMEDCT_US
4040545	VANDF
347100	MMSL
39561	MMSL
d09751	MMSL
018747	NDDF
2550714	RXNORM
2B2VM6UC8G	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
LUMAKRAS	HUMAN PRESCRIPTION DRUG LABEL	1	55513-488	TABLET, COATED	120 mg	ORAL	NDA	30 sections
LUMAKRAS	HUMAN PRESCRIPTION DRUG LABEL	1	55513-504	TABLET, COATED	320 mg	ORAL	NDA	30 sections
LUMAKRAS	HUMAN PRESCRIPTION DRUG LABEL	1	55513-512	TABLET, COATED	240 mg	ORAL	NDA	30 sections

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sotorasib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

Drug Use | Suggest Off label Use Form| |View source of the data|

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: