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DRUG CLASS:

pan-KRAS inhibitor

13d
BBO-11818 in Adult Subjects With KRAS Mutant Cancer (clinicaltrials.gov)
P1, N=387, Recruiting, TheRas, Inc., d/b/a BBOT (BridgeBio Oncology Therapeutics) | N=287 --> 387
Enrollment change • First-in-human
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KRAS (KRAS proto-oncogene GTPase)
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KRAS G12C • KRAS G12D • KRAS G12 • KRAS G12S
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Keytruda (pembrolizumab) • Erbitux (cetuximab) • cisplatin • carboplatin • gemcitabine • 5-fluorouracil • albumin-bound paclitaxel • pemetrexed • oxaliplatin • leucovorin calcium
13d
A Phase I/IIa Study of JAB-23E73 in Patients With Advanced Solid Tumors Harboring KRAS Gene Alteration (clinicaltrials.gov)
P1/2, N=334, Recruiting, Jacobio Pharmaceuticals Co., Ltd. | Trial primary completion date: Dec 2025 --> Dec 2026
Trial primary completion date
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KRAS (KRAS proto-oncogene GTPase)
20d
Enrollment closed • Enrollment change • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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Keytruda (pembrolizumab) • Avastin (bevacizumab) • Erbitux (cetuximab) • cisplatin • carboplatin • gemcitabine • 5-fluorouracil • albumin-bound paclitaxel • pemetrexed • oxaliplatin • leucovorin calcium • sasanlimab (PF-06801591) • PF-07284892
21d
A Study to Test Different Doses of BI 1701963 Alone and Combined With Trametinib in Patients With Different Types of Advanced Cancer (Solid Tumours With KRAS Mutation) (clinicaltrials.gov)
P1, N=71, Active, not recruiting, Boehringer Ingelheim | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
Trial completion date • Trial primary completion date
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation
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Mekinist (trametinib) • BI 1701963
3ms
JAB-23E73 in Adult Participants With Advanced Solid Tumors With KRAS Alteration (clinicaltrials.gov)
P1/2, N=294, Recruiting, Jacobio Pharmaceuticals Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
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KRAS (KRAS proto-oncogene GTPase)
4ms
TLN-372 in Advanced KRAS Mutant Solid Tumors (clinicaltrials.gov)
P1, N=240, Recruiting, Treeline Biosciences, Inc.
New P1 trial
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KRAS (KRAS proto-oncogene GTPase)
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Keytruda (pembrolizumab) • Erbitux (cetuximab)
5ms
Structure-Based Discovery of Active Pan-KRas Inhibitors Targeting G12D Mutants by Enhanced Sampling Simulations. (PubMed, J Phys Chem B)
The anticancer activities of SS-3091 and SS-30125 have been validated against the KRas G12D, G12C, G12V, and G12S mutants in various cancer cells. All findings underscore the potential of SS-3091 and SS-30125 as very promising active pan-KRas inhibitors.
Journal
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS G12C • KRAS G12D • KRAS wild-type • RAS mutation • RAS wild-type • KRAS G12 • KRAS G12S
5ms
An allele-agnostic mutant-KRAS inhibitor suppresses tumor maintenance signals and reprograms tumor immunity in pancreatic cancer. (PubMed, Sci Transl Med)
Here, we comprehensively evaluated the preclinical efficacy of BI-2493, a first-in-class allele-agnostic mutant-KRAS inhibitor (panKRASi), in pancreatic ductal adenocarcinoma (PDAC)...In the long term, emergence of resistance to panKRASi monotherapy was associated with increased YAP signaling within tumor cells and enhanced expression of immune checkpoints in the TME that impede effective T cell function. Our multifaceted approach identified potential combinatorial approaches for generating sustained responses to panKRASi.
Journal
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KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11) • CD8 (cluster of differentiation 8) • AMPK (Protein Kinase AMP-Activated Catalytic Subunit Alpha 1)
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KRAS mutation
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BI-2493
5ms
Enrollment open
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Keytruda (pembrolizumab) • Vectibix (panitumumab)
6ms
A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. (PubMed, Cancer Cell)
MCB-294 also demonstrates superior activity compared to the inactive-state selective pan-KRAS inhibitor Bl-2865 and the KRASG12D inhibitor MRTX1133...Notably, both MCB-294 and MCB-36 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. These findings highlight a promising therapeutic strategy for broadly targeting KRAS-driven tumors and overcoming drug resistance.
Journal
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KRAS (KRAS proto-oncogene GTPase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
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KRAS G12D
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MRTX1133
6ms
BOREALIS-1: A Study of ERAS-4001 in Patients With Advanced or Metastatic Solid Tumors. (clinicaltrials.gov)
P1, N=200, Recruiting, Erasca, Inc. | Not yet recruiting --> Recruiting
Enrollment open
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Keytruda (pembrolizumab) • Vectibix (panitumumab)
6ms
New P1 trial
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Keytruda (pembrolizumab) • Vectibix (panitumumab)