Insilico Medicine AI-discovered drug pipeline. 40+ total programs, 32 preclinical candidates nominated, 13 IND approvals, rentosertib in Phase III, several others in Phase I or IIa, 1 Phase I complete. Zero failures.
First end-to-end generative-AI-designed drug to reach Phase III. Both target and molecule discovered by AI. Positive Phase IIa results published in Nature Medicine (2025); Phase III trial (CTR20262475/NCT07687459) initiated July 7, 2026.
USP1 inhibitor for BRCA-mutant cancers. Out-licensed to Exelixis ($80M upfront + milestones, 2023); Phase I trial ongoing (NCT05932862).
Gut-restricted PHD1/2 inhibitor. Advanced to the BETHESDA Phase IIa trial after positive Phase I results; first patient dosed January 2026.
KAT6 inhibitor for hormone receptor-positive breast cancer. Out-licensed to Menarini/Stemline Therapeutics (up to $500M, 2024); Phase I trial (NCT06638307) ongoing, alone and with elacestrant.
Orally available covalent irreversible 3CLPro inhibitor. Phase I completed.
Glutaminyl-peptide cyclotransferase-like protein inhibitor. Novel immunotherapy for cold tumors.
Oral, systemic PHD inhibitor stabilizing HIF-1alpha to promote erythropoietin production. IND cleared 2023; out-licensed to TaiGen Biotechnology for Greater China (December 2025).
NLRP3 inflammasome inhibitor for inflammatory diseases.
Methionine adenosyltransferase 2α inhibitor. Synthetic lethality for MTAP-deleted cancers.
Ectonucleotide pyrophosphatase/phosphodiesterase 1 inhibitor. Stabilizes cGAMP to activate the cGAS-STING pathway. FDA IND clearance late 2024; Phase I (NCT06724042) underway, alone and with pembrolizumab, cisplatin, or docetaxel.
Pan-TEAD inhibitor for Hippo pathway-driven cancers.
Diacylglycerol kinase A inhibitor. Combination with checkpoint inhibitors.
CDK12 inhibitor to induce BRCAness and sensitize tumors to PARP inhibition.
Dual FGFR2/3 inhibitor for solid tumors.
KIF18A inhibitor targeting chromosomally unstable cancers with TP53 mutations.
WRN helicase inhibitor for microsatellite instability-high cancers.
Potential first-in-class, pipeline-in-a-drug candidate designed with Chemistry42. Nominated as PCC in August 2026, Insilico's 32nd since 2021; designed for oral or eye-drop delivery.
Every program above was discovered using Insilico Medicine's end-to-end generative AI platform: PandaOmics (target discovery), Chemistry42 (generative chemistry), and InClinico (clinical trial prediction).
Source: insilico.com/pipeline · Insilico Medicine public disclosures, clinicaltrials.gov, press releases, and peer-reviewed publications.