adagrasib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Ras protein inhibitors | 5694 | 2326521-71-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Adagrasib is an irreversible inhibitor of KRAS G12C that covalently binds to the mutant cysteine in KRAS G12C and locks the mutant KRAS protein in its inactive state that prevents downstream signaling without affecting wild-type KRAS protein. Adagrasib inhibits tumor cell growth and viability in cells harboring KRAS G12C mutations and results in tumor regression in KRAS G12C-mutated tumor xenograft models with minimal off-target activity.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 12, 2022 | FDA | MIRATI THERAPEUTICS, INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX77 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| MeSH PA | D000970 | Antineoplastic Agents |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 200MG | KRAZATI | MIRATI THERAPS | N216340 | Dec. 12, 2022 | RX | TABLET | ORAL | 10689377 | May 17, 2037 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 200MG | KRAZATI | MIRATI THERAPS | N216340 | Dec. 12, 2022 | RX | TABLET | ORAL | Dec. 12, 2027 | NEW CHEMICAL ENTITY |
| 200MG | KRAZATI | MIRATI THERAPS | N216340 | Dec. 12, 2022 | RX | TABLET | ORAL | Dec. 12, 2029 | 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| GTPase KRas | Enzyme | INHIBITOR | IC50 | 7.85 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEMBL4594350 | ChEMBL_ID |
| C000718190 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10888 | IUPHAR_LIGAND_ID |
| DB15568 | DRUGBANK_ID |
| 019248 | NDDF |
| 4041908 | VANDF |
| C5544276 | UMLSCUI |
| 11519 | INN_ID |
| D12301 | KEGG_DRUG |
| 138611145 | PUBCHEM_CID |
| 2625882 | RXNORM |
| 364307 | MMSL |
| 41146 | MMSL |
| d09956 | MMSL |
| 8EOO6HQF8Y | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| KRAZATI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 80739-812 | TABLET, COATED | 200 mg | ORAL | NDA | 29 sections |