Table 1 Direct KRAS inhibitors undergoing clinical trials
From: MYC and KRAS cooperation: from historical challenges to therapeutic opportunities in cancer
Inhibitor | Treatment strategy | Indication | Sponsor | Stage | Trial identifier |
|---|---|---|---|---|---|
G12C inhibitors | |||||
Sotorasib (AMG 510) | Monotherapy | Solid tumors | Amgen | Phase I/II | NCT03600883 |
NSCLC | Amgen | Phase II | NCT04933695 | ||
NSCLC | Vestre Viken Hospital Trust | Phase II | NCT05311709 | ||
NSCLC | Fundación GECP | Phase II | NCT05398094 | ||
NSCLC | Gustave Roussy | Phase II | NCT05631249 | ||
Non-squamous NSCLC | SWOG Cancer Research Network | Phase II | NCT04625647 | ||
NSCLC | Amgen | Phase III | NCT04303780 | ||
NSCLC | Memorial Sloan Kettering Cancer Center | Phase II | NCT06333678 | ||
Combination with stereotactic radiation therapy | Brain metastasis from NSCLC | Karolinska University Hospital | Phase I | NCT06127940 | |
Combination with SHP2 inhibitor | NSCLC; solid tumors | Navire Pharma Inc | Phase I | NCT05480865 | |
Combination with six other therapies | MTAP-deleted thoracic tumors | Amgen | Phase I | NCT06333951 | |
Combination with carfilzomib | NSCLC | City of Hope Medical Center | Phase I | NCT06249282 | |
Combination with tarloxotinib | NSCLC | Medical University of South Carolina | Phase Ib | NCT05313009 | |
Combination with ladaraxin | NSCLC | NYU Langone Health | Phase I/II | NCT05815173 | |
Combination with avutometinib | NSCLC | Verastem Inc | Phase I/II | NCT05074810 | |
Combination with DCC-3116 | Solid tumors | Deciphera Pharmaceuticals LLC | Phase I/II | NCT04892017 | |
Combination with JAB-3312 | Solid tumors; NSCLC | Jacobio Pharmaceuticals Co., Ltd | Phase I/II | NCT04720976 | |
Combination with zotatifin (eFT226) | Solid tumors | Effector Therapeutics | Phase I/II | NCT04092673 | |
Combination with 13 other anti-cancer therapies | Solid tumors | Amgen | Phase I/II | NCT04185883 | |
Combination with cisplatin (or carboplatin) and pemetrexed chemotherapy | Non-squamous NSCLC | M.D. Anderson Cancer Center | Phase II | NCT05118854 | |
Combination with RMC-4630 | NSCLC | Revolution Medicines, Inc. | Phase II | NCT05054725 | |
Combination with panitumumab | Solid tumors | Korea University Anam Hospital | Phase II | NCT05993455 | |
Combination with panitumumab | Solid tumors | National Cancer Institute (NCI) | Phase II | NCT05638295 | |
Combination with 15 cancer therapies | Solid tumors | National Cancer Institute (NCI) | Phase II | NCT05564677 | |
Combination with platinum doublet chemotherapy (against pembrolizumab with platinum doublet chemotherapy) | NSCLC | Amgen | Phase III | NCT05920356 | |
Combination with panitumumab and FOLFIRI | CRC | Amgen | Phase III | NCT06252649 | |
Combination with panitumumab | CRC | Amgen | Phase III | NCT05198934 | |
Adagrasib (MRTX849) | Monotherapy | Solid Tumors | Zai Lab (Shanghai) Co., Ltd | Phase I | NCT05263986 |
PDAC | M.D. Anderson Cancer Center | Phase Ib | NCT05634525 | ||
Solid Tumors | Mirati Therapeutics Inc. | Phase I/II | NCT03785249 | ||
NSCLC | ETOP IBCSG Partners Foundation | Phase II | NCT05673187 | ||
Solid tumors; malignant neoplasms of lung | Mirati Therapeutics Inc | Phase II | NCT05853575 | ||
NSCLC | Mirati Therapeutics Inc. | Phase III | NCT04685135 | ||
Combination with INCB099280 | Solid tumors | Incyte Corporation | Phase I | NCT06039384 | |
Combination with KO-2806 | Solid tumors | Kura Oncology, Inc. | Phase I | NCT06026410 | |
Combination with palbociclib | Solid tumors | Mirati Therapeutics Inc. | Phase I | NCT05178888 | |
Combination with cetuximab and irinotecan | CRC | M.D. Anderson Cancer Center | Phase I | NCT05722327 | |
Combination with olaparib | Solid tumors | M.D. Anderson Cancer Center | Phase Ib | NCT06130254 | |
Combination with nab-sirolimus | NSCLC; solid tumors | Mirati Therapeutics Inc. | Phase I/II | NCT05840510 | |
Combination with MRTX0902 | Solid tumors | Mirati Therapeutics Inc. | Phase I/II | NCT05578092 | |
Combination with TNO155 | Solid tumors | Mirati Therapeutics Inc. | Phase I/II | NCT04330664 | |
Combination with BMS-986466 with or without cetuximab | Solid Tumors | Bristol-Myers Squibb | Phase I/II | NCT06024174 | |
Combination with avutometinib | NSCLC | Verastem, Inc. | Phase I/II | NCT05375994 | |
Combination with SAR442720 | Solid tumors | Sanofi | Phase I/II | NCT04418661 | |
Combination with pembrolizumab and cisplatin/carboplatin plus pemetrexed | NSCLC | Mirati Therapeutics Inc. | Phase II | NCT05609578 | |
Monotherapy and in combination with nivolumab | Resectable NSCLC | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Phase II | NCT05472623 | |
Combination with stereotactic radiation therapy | Brain metastasis from NSCLC | Ryan Gentzler, MD | Phase II | NCT06248606 | |
Monotherapy and in combination with pembrolizumab | NSCLC | Mirati Therapeutics Inc | Phase II/III | NCT04613596 | |
Combination with cetuximab | CRC | Mirati Therapeutics Inc. | Phase III | NCT04793958 | |
Opnurasib (JDQ443) | Monotherapy | NSCLC | Novartis Pharmaceuticals | Phase II | NCT05445843 |
NSCLC | Canadian Cancer Trials Group | Phase II | NCT05714891 | ||
NSCLC with brain metastasis | Maastricht University Medical Center | Phase II | NCT05999357 | ||
NSCLC | Novartis Pharmaceuticals | Phase III | NCT05132075 | ||
Monotherapy and in combination with TNO155 and tislelizumab | Solid tumors | Novartis Pharmaceuticals | Phase Ib/II | NCT04699188 | |
Combination with trametinib, ribociclib and cetuximab | Solid tumors | Novartis Pharmaceuticals | Phase Ib/II | NCT05358249 | |
Divarasib (GDC-6036) | Monotherapy | Solid tumors | Genentech, Inc. | Phase I | NCT04449874 |
NSCLC | Genentech, Inc. | Phase II | NCT04302025 | ||
NSCLC | Hoffmann-La Roche | Phase II/III | NCT03178552 | ||
Combination with eight other anti-cancer treatments | CRC | Hoffmann-La Roche | Phase I | NCT04929223 | |
Combination with pembrolizumab, carboplatin, cisplatin and pemetrexed | NSCLC | Hoffmann-La Roche | Phase I/II | NCT05789082 | |
Combination with eight other anti-cancer treatments | Solid tumors | Hoffmann-La Roche | Phase II | NCT04589845 | |
LY3537982 | Monotherapy | Solid tumors | Eli Lilly and Company | Phase I | NCT04956640 |
Solid tumors | Eli Lilly and Company | Phase I | NCT06235983 | ||
In combination with pembrolizumab, cisplatin, carboplatin and pemetrexed | NSCLC | Eli Lilly and Company | Phase III | NCT06119581 | |
BI-1823911 | Monotherapy and in combination with BI-1701963 | Solid tumors | Boehringer Ingelheim | Phase Ia/Ib | NCT04973163 |
RMC-6291 | Monotherapy | Solid tumors | Revolution Medicines, Inc. | Phase I | NCT05462717 |
Combination with RMC-6236 | Solid tumors | Revolution Medicines, Inc. | Phase I | NCT06128551 | |
Combination with RMC-6236 or with SOC | Solid tumors with a focus on NSCLC | Revolution Medicines, Inc. | Phase I/II | NCT06162221 | |
D-1553 | Monotherapy | NSCLC | InventisBio Co., Ltd | Phase I/II | NCT05383898 |
NSCLC | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Phase III | NCT06300177 | ||
Monotherapy and in combination with SoC (not determined) | Solid tumors | InventisBio Co., Ltd | Phase I/II | NCT04585035 | |
Combination with IN10018 | Solid tumors | InventisBio Co., Ltd | Phase I/II | NCT05379946 | |
Combination with IN10018 | Solid tumors | InxMed (Shanghai) Co., Ltd. | Phase I/II | NCT06166836 | |
In combination with SoC (not determined) | NSCLC | InventisBio Co., Ltd | Phase Ib/II | NCT05492045 | |
JAB-21822 | Monotherapy | Solid tumors | Jacobio Pharmaceuticals Co., Ltd. | Phase I/II | NCT05009329 |
NSCLC | Jacobio Pharmaceuticals Co., Ltd. | Phase I/II | NCT05276726 | ||
PDAC | Jacobio Pharmaceuticals Co., Ltd. | Phase II | NCT06008288 | ||
Combination with JAB-3312 | Solid tumors | Jacobio Pharmaceuticals Co., Ltd. | Phase I/II | NCT05288205 | |
Monotherapy and in combination with cetuximab | Solid tumors | Jacobio Pharmaceuticals Co., Ltd. | Phase I/II | NCT05194995 | |
Monotherapy and in combination with cetuximab | Solid tumors | Jacobio Pharmaceuticals Co., Ltd. | Phase I/II | NCT05002270 | |
G12D inhibitors | |||||
MRTX1133 | Monotherapy | Solid tumors | Mirati Therapeutics Inc. | Phase I/II | NCT05737706 |
RMC-9805 | Monotherapy | Solid tumors | Revolution Medicines, Inc. | Phase I | NCT06040541 |
ASP3082 | Monotherapy and in combination with cetuximab | Solid tumors | Astellas Pharma Inc | Phase I | NCT05382559 |
HRS-4642 | Monotherapy | Solid tumors | Jiangsu HengRui Medicine Co., Ltd. | Phase I | NCT05533463 |
INCB161734 | Monotherapy and in combination with cetuximab or retifanlimab | Solid tumors | Incyte Corporation | Phase I | NCT05533463 |
