Treeline Biosciences

Updated: February 01, 2026
Founders: Josh Bilenker, Jeffrey Engelman
Founders: Josh Bilenker, Jeffrey Engelman
Country: USA | Funding: $1.1B (+)
Founded: 2021

Website: https://treeline.bio

Treeline Biosciences develops oral small molecules for precision treatment of cancer. It also creates protein splitters and "stickers" for situations where traditional small molecules are unlikely to be effective, focusing on pharmacology from the outset. For drug delivery, the company uses antibody-tagged conjugates (TT-ADCs), an elegant solution that avoids exposure to healthy tissues. Treeline is conducting clinical trials of two drugs for the treatment of lymphoma: TLN-121 (in-house developed), which disrupts the BCL6 protein, and TLN-254 (licensed from Hengrui Pharmaceuticals), which inhibits the EZH2 protein. The company has also begun clinical trials of a pan-KRAS inhibitor, TLN-372, for the treatment of solid tumors with certain KRAS mutations.

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