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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.
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.
Investors not recorded; see the round sources.
| Round | Year | Amount | Source |
|---|---|---|---|
| Series A · Series A total including the A2 extension led by GGV Capital, with Pavilion Capital, Cenova Capital, Mitsui & Co. Global Investment and CBC Group. | 2022 | $67M | ensemtx.com |
Amounts only where the cited source states them. Rounds without a public source are not listed.
Shares PI3K, AKT and mTOR inhibitors, PIK3CA / PI3K-alpha, Breast cancer (all types).
Shares PI3K, AKT and mTOR inhibitors, PIK3CA / PI3K-alpha, HR-positive / HER2-negative breast cancer.
Shares PI3K, AKT and mTOR inhibitors, KRAS, Breast cancer (all types).
Shares PIK3CA / PI3K-alpha, KRAS, HR-positive / HER2-negative breast cancer.
Shares PI3K, AKT and mTOR inhibitors, HR-positive / HER2-negative breast cancer.
Shares PIK3CA / PI3K-alpha, AI-driven drug & target discovery, HR-positive / HER2-negative breast cancer.
Shares PI3K, AKT and mTOR inhibitors, PIK3CA / PI3K-alpha, HR-positive / HER2-negative breast cancer.
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