Pipeline

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

Our programs are grounded in rational science 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 inhibitor of KRASG12C that is optimized to sustain target inhibition. This attribute could be important to treat KRASG12C mutated cancers, as the KRASG12C protein regenerates every 24 to 48 hours.

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.

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

MRTX1719 is an investigational, internally discovered synthetic lethal PRMT5 inhibitor for the treatment of methylthioadenosine phosphorylase (MTAP)-deleted cancers.

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
IND-Enabling
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.