Adagrasib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2022
- First approval year
- 2022
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Adagrasib
- Molecular weight
- 604.13
- Structure (SMILES)
- C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
- krazati
- Krazati
- adagrasib
- Adagrasib
- ADAGRASIB
- adagrasib (MRTX849)
- ADAGRASIB (MRTX849)
- adagrasib [INN]
- Adagrasib [MI]
- ADAGRASIB [USAN]
- Adagrasib [WHO-DD]
- adagrasib inn
- adagrasib mi
- adagrasib mrtx849
- adagrasib usan
- adagrasib who dd
- compound 20
- COMPOUND 20
- kras g12c inhibitor mrtx849
- Kras g12c inhibitor mrtx849
- KRAS G12C INHIBITOR MRTX849
- krazati
- Krazati
- KRAZATI
- mrtx 849
- Mrtx-849
- MRTX-849
And 3 more, listed on the interactive page.
- ATC classification codes
- L01XX77
Sources for recorded values
- CAS registry numbers
- 2326521-71-3
- ChEMBL ID
- CHEMBL4594350
- InChIKey
- PEMUGDMSUDYLHU-ZEQRLZLVSA-N
- PubChem compound IDs
- 138611145
- RxNorm IDs (RxCUI)
- 2625882
- FDA ingredient codes (UNII)
- 8EOO6HQF8Y
- Applicant
- BRISTOL
- Approval date
- 12 Dec 2022
- Application number
- NDA216340
- Status
- Authorised
- Status date
- 5 Jan 2024
- Authorisation date
- 5 Jan 2024
- Approved indications
- Krazati as monotherapy is indicated for the treatment of adult patients with advanced non-small cell lung cancer (NSCLC) with KRAS G12C mutation and disease progression after at least one prior systemic therapy.
- Product number
- EMEA/H/C/006013
- Authorisation holder
- Bristol-Myers Squibb Pharma EEIG
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- Yes
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Carcinoma, Non-Small-Cell Lung
European medicines record
- Patents
- 4
- Designations
- 7
- Earliest recorded loss of exclusivity
- 21 Aug 2043
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- adagrasib
- Type
- Synthetic organic
- Drug name stem
- -rasib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KRAS
- Gene symbol
- KRAS
- Protein identifier
- P01116
- Median affinity
- 5.43
- Affinity units
- pKi
- Mechanism
- GTPase KRas inhibitor
- Action type
- Inhibitor
- Target
- GTPase KRas
- Protein identifier
- P01116
Open Targets mechanisms
- Mechanism
- GTPase KRas inhibitor
- Action type
- Inhibitor
- Target
- GTPase KRas
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Neoplasm Metastasis
- Highest recorded phase
- 1
- Condition identifier
- EFO:0009709
- Subject identifier
- D009362
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000359
- Subject identifier
- D010190
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Lung Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_1000359
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005184
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008903
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0024880
Reported adverse events
- Event
- skin hyperpigmentation
- Reports
- 1
- Reporting signal score
- 5.91138
- NCT04418661
- NCT05178888
- NCT05263986
- NCT06024174
- NCT06039384
- NCT05472623
- NCT05609578
- NCT05673187
- NCT06130254
- NCT06248606
- NCT05634525
- NCT05722327
- NCT05848843
- Dose
- 600 mg
- Route
- Oral
- How often
- Twice daily
- Swallow tablets whole
- Take with or without food
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 0
- Polar surface area
- 88.83
- Calculated partition coefficient (ALogP)
- 4.73
- Calculated partition coefficient (XLogP)
- 5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 7
- Heavy atoms
- 43
- Molecular formula
- C32H35ClFN7O2
- Monoisotopic mass
- 603.2524792
- Natural product
- No
- 80739-812
- Recorded assays
- 308
- Active assays
- 65
Active assay types
- Confirmatory
- Antineoplastic Agents
These details could not be displayed.
Related records
Trials (38)
- A Multicenter Phase 1b/2 Study of Adagrasib, Cetuximab, and Cemiplimab for Metastatic Colorectal Cancer Harboring KRAS G12C Mutations
- A Phase 1 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway
- A Phase I Study of Adagrasib and Durvalumab for Treatment of Advanced Non-small Cell Lung Cancers and Gastro-intestinal Cancers Harboring KRAS G12C Mutations
- A PK Study to Assess the Drug-drug Interaction of a BCRP Inhibitor on Adagrasib
- A Solid Tumor Study for Long Term Treatment of Cancer Patients Who Participated in Adagrasib Studies
- A Study Evaluating the Efficacy and Safety of Divarasib Versus Sotorasib or Adagrasib in Participants With Previously Treated KRAS G12C-positive Advanced or Metastatic Non-Small Cell Lung Cancer
- A Study of Adagrasib Plus Pembrolizumab Plus Chemotherapy vs. Placebo Plus Pembrolizumab Plus Chemotherapy in Participants With Previously Untreated Non-squamous Non-small Cell Lung Cancer With KRAS G12C Mutation (KRYSTAL-4)
- A Study of BMS-986466 With Adagrasib With or Without Cetuximab in Participants With Kirsten Rat Sarcoma Virus Glycine 12 to Cysteine (KRAS G12C)-Mutant Solid Tumors
- A Study of BMS-986488 as Monotherapy and Combination Therapy in Participants With Advanced Malignant Tumors
- A Study of INCB099280 in Combination With Adagrasib in Adults With Advanced Solid Tumors Harboring a KRASG12C Mutation
- A Study to Assess the Pharmacokinetics, Safety and Tolerability of Single-dose Adagrasib (BMS-986503) in Healthy Participants of Japanese Descent
- Adagrasib + SRS for Patients With Metastatic KRAS G12C-mutated NSCLC With Untreated Brain Metastases
- Adagrasib in Combination With BI 1701963 in Patients With Cancer (KRYSTAL 14)
- Adagrasib in Combination With Nab-Sirolimus in Patients With Advanced Solid Tumors and Non-Small Cell Lung Cancer With a KRAS G12C Mutation (KRYSTAL -19)
- Adagrasib in Combination With Palbociclib in Patients With Advanced Solid Tumors (KRYSTAL-16)
- Adagrasib in Combination With TNO155 in Patients With Cancer (KRYSTAL 2)
- Adagrasib in Patients With KRASG12C-mutant NSCLC Who Are Elderly or Have Poor Performance Status
- ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer
- Bioequivalence Study Between Adagrasib Reference Tablets and High Drug Load Tablets
- CIMAvax-EGF With KRAS G12C Inhibitor for the Treatment of Advanced, KRAS G12C Mutated Non Small Cell Lung Cancer
Approved for (2)
- Neoplasm
- Non-small cell lung carcinoma
In development for (4)
- Colorectal cancer Phase 1
- Lung cancer Phase 1
- Malignant pancreatic neoplasm Phase 1
- Metastatic neoplasm Phase 1
Other linked conditions (2)
Targets (1)
- KRAS GTPase KRas inhibitor