Pipeline

Mirati is developing a pipeline of novel therapeutics that directly target the genetic and immunological drivers of cancer to ultimately help improve the lives of patients with cancer.

Mirati is developing a pipeline of novel therapeutics that directly target the genetic and immunological drivers of cancer to ultimately help improve the lives of patients with cancer.

Each of our programs is based on a scientific rationale to identify and treat patients most likely to respond to Mirati’s targeted therapies. Click on each program to learn more.

Adagrasib (MRTX849)
KRASG12C Inhibitor

Adagrasib (MRTX849) is an investigational, highly selective and potent, oral small-molecule therapy designed to shrink difficult-to-treat cancers harboring the KRASG12C mutation.

Development
Approach
Lead
Optimization
IND-Enabling
Phase 1/1b
Phase 2
Phase 3
Monotherapy
KRYSTAL-1: 2L+ NSCLC, CRC, Pancreatic, Other
Phase 2
KRYSTAL-1: 1L NSCLC STK11 Co-Mutation Cohort
Phase 2
KRYSTAL-12: 2L NSCLC (Randomized to Docetaxel)
Phase 3
Combination with Pembrolizumab (PD-1)
KRYSTAL-7: 1L NSCLC (2 Combination Arms <1% TPS and ≥1% TPS)
Phase 2
Combination with Cetuximab (EGFR)
KRYSTAL-10: 2L CRC (Randomized to FOLFIRI or FOLFOX)
Phase 3
POC Combinations: SHP2, SOS1, Pan-EGFR, CDK4/6
2L+ NSCLC and CRC (Multiple Proof of Concept Combination Trials)
Phase 2
MRTX1133
KRASG12D Inhibitor

MRTX1133 is an investigational, highly selective and potent small molecule-inhibitor of the KRASG12D mutation, designed to treat patients with high unmet need.

Development
Approach
Lead
Optimization
IND-Enabling
Phase 1/1b
Phase 2
Phase 3
Monotherapy
Pancreatic, CRC, NSCLC, Other
IND-Enabling
Sitravatinib
Multi Kinase Inhibitor

Sitravatinib is an investigational spectrum-selective receptor tyrosine kinase (RTK) inhibitor that can potentially stimulate the body’s immune response to fight cancer.

Development
Approach
Lead
Optimization
IND-Enabling
Phase 1/1b
Phase 2
Phase 3
PD-1
2/3L NS-NSCLC (SAPPHIRE – Combination with Nivolumab vs. Docetaxel)
Phase 3
P3 2/3L S + NS-NSCLC; combination studies in other solid tumors1
Phase 2
MRTX1719
Synthetic Lethal PRMT5 Inhibitor
Development
Approach
Lead
Optimization
IND-Enabling
Phase 1/1b
Phase 2
Phase 3
Monotherapy
MTAP-Deleted Cancers
IND-Enabling
Discovery Programs
Development
Approach
Lead
Optimization
IND-Enabling
Phase 1/1b
Phase 2
Phase 3
SOS1 Inhibitor (KRAS Signal Modifying)
Solid Tumors
Lead Optimization
Mutant KRAS Inhibitor
Solid Tumors
Lead Optimization

POC = proof of concept; P = Phase; L= Line; NSCLC = non-small cell lung cancer; CRC = colorectal cancer; OS = overall survival; IND = investigational new drug; NDA = new drug application; TPS = tumor proportion score; BID = twice daily dosing; ORR = objective response rate; MTAP = methylthioadenosine phosphorylase; CNS = central nervous system; S = squamous; NS = non-squamous.

1. BeiGene is currently conducting certain combination studies of sitravatinib + tislelizumab for solid tumor indications in their territory in Asia (ex-Japan). These trials include a P3 trial in non-squamous and squamous NSCLC randomized vs. docetaxel, as well as proof-of-concept trials in hepatocellular carcinoma, renal cell carcinoma, ovarian cancer and gastric.