Adagrasib

Generic Name: Adagrasib

Brand Names: Krazati

Drug Type: Small Molecule

Chemical Formula: C_₃₂H_₃₅ClFN_₇O_₂

CAS Number: 2326521-71-3

Unique Ingredient Identifier: 8EOO6HQF8Y

Background: Adagrasib (MRTX849) is an oral, small-molecule KRAS inhibitor developed by Mirati Therapeutics. KRAS mutations are highly common in cancer and account for approximately 85% of all RAS family mutations. However, the development of KRAS inhibitors has been challenging due to their high affinity for guanosine triphosphate (GTP) and guanosine diphosphate (GDP), as well as the lack of a clear binding pocket. Adagrasib targets KRAS, one of the most common KRAS mutations, at the cysteine 12 residue and inhibits KRAS-dependent signalling. In a phase I/IB clinical study that included patients with KRAS-mutated advanced solid tumors (NCT03785249), adagrasib exhibited anti-tumor activity. The phase II of the same study showed that in patients with KRAS-mutated non-small-cell lung cancer (NSCLC), adagrasib was efficient without new safety signals.

In February 2022, the FDA accepted a new drug application (NDA) for adagrasib for the treatment of patients with previously treated KRAS–positive NSCLC. In December 2022, the FDA granted accelerated approval to adagrasib for the treatment of KRAS-mutated locally advanced or metastatic NSCLC who have received at least one prior systemic therapy. Adagrasib joins sotorasib as another KRAS inhibitor approved by the FDA.

Indication: Adagrasib is 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.

This indication is approved under accelerated approval based on objective response rate (ORR) and duration of response (DOR). Continued approval for this indication may be contingent upon verification and description of a clinical benefit in a confirmatory trial(s).

Associated Conditions: Locally Advanced Non-Small Cell Lung Cancer, Metastatic Non-Small Cell Lung Cancer

Clinical Trials

The Clinical Trial to Evaluate the Pharmacokinetics and Safety of MRTX849 in Patients With Advanced Solid Tumors

Phase 1

Active, not recruiting

Conditions: Advanced or Metastatic Solid Tumor

Interventions: Drug: MRTX849

First Posted Date: 2022-03-03

Last Posted Date: 2023-02-27

Lead Sponsor: Zai Lab (Shanghai) Co., Ltd.

Target Recruit Count: 22

Registration Number: NCT05263986

Locations: 🇨🇳
Chongqing University Cancer Hospital, Chongqing, Chongqing, China
🇨🇳
Henan Cancer Hospital, Zhengzhou, Henan, China
🇨🇳
Beijing Cancer Hospital, Beijing, Beijing, China

and more 5 locations

Adagrasib in Combination With Palbociclib in Patients With Advanced Solid Tumors (KRYSTAL-16)

Phase 1

Completed

Conditions: Advanced Solid Tumor

Interventions: Drug: MRTX849
Drug: Palbociclib

First Posted Date: 2022-01-05

Last Posted Date: 2025-02-11

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 11

Registration Number: NCT05178888

Locations: 🇺🇸
Local Institution - 803, Nashville, Tennessee, United States
🇺🇸
Local Institution - 804, Orlando, Florida, United States
🇺🇸
Local Institution - 802, Houston, Texas, United States

and more 1 locations

Expanded Access of Adagrasib (MRTX849) in Patients With Advanced Solid Tumors Who Have a KRAS G12C Mutation

Conditions: Advanced Cancer
Metastatic Cancer
Malignant Neoplasm

First Posted Date: 2021-12-17

Last Posted Date: 2023-05-19

Lead Sponsor: Mirati Therapeutics Inc.

Registration Number: NCT05162443

Locations: 🇺🇸
Piedmont Cancer Institute, Atlanta, Georgia, United States
🇺🇸
Renown Health, Reno, Nevada, United States
🇺🇸
Lehigh Valley Cancer Institute, Allentown, Pennsylvania, United States

and more 8 locations

Adagrasib in Combination With BI 1701963 in Patients With Cancer (KRYSTAL 14)

Phase 1

Terminated

Conditions: Malignant Neoplasm of Lung
Metastatic Cancer
Malignant Neoplasm of Colon
Advanced Cancer
Malignant Neoplastic Disease

Interventions: Drug: MRTX849
Drug: BI 1701963

First Posted Date: 2021-07-23

Last Posted Date: 2024-12-16

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 7

Registration Number: NCT04975256

Locations: 🇺🇸
Washington University School of Medicine, Saint Louis, Missouri, United States
🇺🇸
The Cleveland Clinic Foundation, Cleveland, Ohio, United States
🇺🇸
Next Oncology, San Antonio, Texas, United States

and more 1 locations

Phase 3 Study of MRTX849 With Cetuximab vs Chemotherapy in Patients With Advanced Colorectal Cancer With KRAS G12C Mutation (KRYSTAL-10)

Phase 3

Active, not recruiting

Conditions: Metastatic Colorectal Cancer
Advanced Colorectal Cancer

Interventions: Drug: MRTX849
Drug: mFOLFOX6 Regimen
Drug: FOLFIRI Regimen
Biological: Cetuximab

First Posted Date: 2021-03-11

Last Posted Date: 2025-02-11

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 461

Registration Number: NCT04793958

Locations: 🇰🇷
Local Institution - 010-116, Anyang-si, Korea, Republic of
🇰🇷
Local Institution - 010-111, Busan, Korea, Republic of
🇰🇷
Local Institution - 010-100, Hwasun-gun, Korea, Republic of

and more 416 locations

Phase 3 Study of MRTX849 (Adagrasib) vs Docetaxel in Patients With Advanced Non-Small Cell Lung Cancer With KRAS G12C Mutation

Phase 3

Active, not recruiting

Conditions: Metastatic Non Small Cell Lung Cancer
Advanced Non Small Cell Lung Cancer

Interventions: Drug: MRTX849
Drug: Docetaxel

First Posted Date: 2020-12-28

Last Posted Date: 2025-01-22

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 453

Registration Number: NCT04685135

Locations: 🇺🇸
Local Institution - 012-898, Cerritos, California, United States
🇺🇸
Local Institution - 012-898 D, Glendale, California, United States
🇺🇸
Local Institution - 012-910-A, Huntington Beach, California, United States

and more 340 locations

Phase 2 Trial of Adagrasib Monotherapy and in Combination With Pembrolizumab and a Phase 3 Trial of Adagrasib in Combination in Patients With a KRAS G12C Mutation KRYSTAL-7

Phase 2

Recruiting

Conditions: Advanced Non-Small Cell Lung Cancer
Metastatic Non-Small Cell Lung Cancer

Interventions: Drug: Adagrasib
Drug: Pembrolizumab

First Posted Date: 2020-11-03

Last Posted Date: 2025-05-21

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 806

Registration Number: NCT04613596

Locations: 🇩🇪
Local Institution - 007-225, Jena, Germany
🇺🇸
Local Institution - 007-556-A, Goodyear, Arizona, United States
🇺🇸
USOR - Arizona Oncology - Prescott Valley, Prescott Valley, Arizona, United States

and more 710 locations

Safety and Efficacy Study of SAR442720 in Combination With Other Agents in Advanced Malignancies

Phase 1

Terminated

Conditions: Metastatic Neoplasm

Interventions: Drug: SAR442720
Drug: Pembrolizumab
Drug: Adagrasib

First Posted Date: 2020-06-05

Last Posted Date: 2025-04-20

Lead Sponsor: Sanofi

Target Recruit Count: 65

Registration Number: NCT04418661

Locations: 🇦🇷
Investigational Site Number : 0320003, Rosario, Santa Fe, Argentina
🇦🇷
Investigational Site Number : 0320001, Buenos Aires, Argentina
🇦🇷
Investigational Site Number : 0320002, Buenos Aires, Argentina

and more 17 locations

Adagrasib in Combination With TNO155 in Patients With Cancer (KRYSTAL 2)

Phase 1

Completed

Conditions: Advanced Cancer
Metastatic Cancer
Malignant Neoplastic Disease

Interventions: Drug: MRTX849
Drug: TNO155

First Posted Date: 2020-04-01

Last Posted Date: 2025-04-04

Lead Sponsor: Mirati Therapeutics Inc.

Target Recruit Count: 86

Registration Number: NCT04330664

Locations: 🇺🇸
Local Institution - 002-803, Orange, California, United States
🇺🇸
Local Institution - 002-942, Wichita, Kansas, United States
🇺🇸
Local Institution - 002-809, Saint Louis, Missouri, United States

and more 14 locations

Genetic Testing in Guiding Treatment for Patients With Brain Metastases

Phase 2

Recruiting

Conditions: Metastatic Malignant Neoplasm in the Brain
Metastatic Malignant Solid Neoplasm
PI3K Gene Mutation
KRAS G12C Mutation
NTRK Family Gene Mutation
CDK Gene Mutation
ROS1 Gene Mutation

Interventions: Drug: Entrectinib
Drug: PI3K Inhibitor paxalisib
Drug: Abemaciclib
Drug: Adagrasib

First Posted Date: 2019-06-21

Last Posted Date: 2025-04-02

Lead Sponsor: Alliance for Clinical Trials in Oncology

Target Recruit Count: 186

Registration Number: NCT03994796

Locations: 🇺🇸
Anchorage Radiation Therapy Center, Anchorage, Alaska, United States
🇺🇸
Anchorage Associates in Radiation Medicine, Anchorage, Alaska, United States
🇺🇸
Katmai Oncology Group, Anchorage, Alaska, United States

and more 433 locations

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