{"entity":{"id":"ensem-therapeutics","kind":"company","name":"Ensem Therapeutics","aka":[],"tldr":"Ensem Therapeutics designs small-molecule medicines with computer modelling. Its lead drug, ETX-636, blocks a faulty version of the PI3K-alpha protein and is in an early trial in advanced breast cancer and other solid tumours.","summary":"Ensem Therapeutics, headquartered in Waltham, Massachusetts, with a site in Shanghai, uses its Kinetic Ensemble platform, which applies AI and machine learning to structural ensemble-based drug design, to develop small-molecule precision medicines. The company was incubated by CBC Group from 2021 and reported a Series A total of USD 67 million in April 2022, after a Series A2 led by GGV Capital. Its lead, ETX-636, is described as an allosteric, pan-mutant-selective PI3K-alpha inhibitor and degrader designed to spare glucose homeostasis; first patient dosing in the global phase 1/2 study (NCT06993844), alone and with fulvestrant, was announced in July 2025, it received FDA Fast Track designation for advanced breast cancer in October 2025, and a first patient was dosed in China in February 2026. Preclinical programmes include ETX-929 (pan-KRAS), ETX-880 (covalent WRN helicase inhibitor for MSI-high cancers) and ETX-197 (CDK2), and in November 2023 it partnered a CDK2 inhibitor with BeiGene. Its first registered cancer trial as sponsor, NCT06993844, was posted on ClinicalTrials.gov in May 2025.","asOf":"2026-10-29","links":[{"label":"Official website","url":"https://ensemtx.com/"},{"label":"Pipeline","url":"https://ensemtx.com/science/pipeline/"},{"label":"Series A release, April 2022","url":"https://ensemtx.com/ensem-therapeutics-a-cbc-group-incubated-biopharma-company-raises-67-million-in-series-a-financing-to-develop-small-molecule-medicines-for-difficult-to-drug-targets-2/"}],"tags":[],"related":[],"cancers":["breast-cancer","breast-hr-positive"],"sections":["targeted-therapy","ai-computation"],"technologies":["pi3k-akt-mtor-inhibitors","ai-drug-design"],"targets":["pik3ca","kras","wrn","cdk2"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct06993844"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["Founding year not stated; the company says it was incubated by CBC Group since 2021.","A June 2024 release reports a milestone when a CDK2 inhibitor entered trials; that programme was partnered with BeiGene and is not an Ensem-sponsored registry study.","Company pipeline, news page and Series A release read on 29 October 2026."],"hq":"Waltham, MA","country":"US","companyType":"biotech","website":"https://ensemtx.com/","stage":"growth","investors":[],"funding":[{"round":"Series A","year":2022,"amountUsd":67000000,"source":"https://ensemtx.com/ensem-therapeutics-a-cbc-group-incubated-biopharma-company-raises-67-million-in-series-a-financing-to-develop-small-molecule-medicines-for-difficult-to-drug-targets-2/","note":"Series A total including the A2 extension led by GGV Capital, with Pavilion Capital, Cenova Capital, Mitsui & Co. Global Investment and CBC Group."}]},"route":"/companies/ensem-therapeutics/","neighbours":{"cancer":[{"id":"breast-cancer","kind":"cancer","name":"Breast cancer (all types)","route":"/cancers/breast-cancer/"},{"id":"breast-hr-positive","kind":"cancer","name":"HR-positive / HER2-negative breast cancer","route":"/cancers/breast-hr-positive/"}],"section":[{"id":"ai-computation","kind":"section","name":"AI & Computation","route":"/fronts/ai-computation/"},{"id":"targeted-therapy","kind":"section","name":"Targeted Therapy","route":"/fronts/targeted-therapy/"}],"technology":[{"id":"ai-drug-design","kind":"technology","name":"AI-driven drug & target discovery","route":"/technologies/ai-drug-design/"},{"id":"pi3k-akt-mtor-inhibitors","kind":"technology","name":"PI3K, AKT and mTOR inhibitors","route":"/technologies/pi3k-akt-mtor-inhibitors/"}],"target":[{"id":"cdk2","kind":"target","name":"CDK2","route":"/targets/cdk2/"},{"id":"kras","kind":"target","name":"KRAS","route":"/targets/kras/"},{"id":"pik3ca","kind":"target","name":"PIK3CA / PI3K-alpha","route":"/targets/pik3ca/"},{"id":"wrn","kind":"target","name":"WRN helicase (MSI-high cancers)","route":"/targets/wrn/"}],"trial":[{"id":"nct06993844","kind":"trial","name":"Phase 1/2 Study of ETX-636 in Participants With Advanced Solid Tumors","route":"/trials/nct06993844/"}]}}