Drug intelligence / Profile preview

tirbanibulin + paclitaxel

Development stage
Unknown
Lead developer
Athenex
Modality
Small Molecules
Administration
Oral, Topical, Intravenous
01

Overview

Tirbanibulin (KX2-391) is a synthetic, orally active small molecule that acts as a dual inhibitor of Src tyrosine kinase signaling and tubulin polymerization. It induces p53 expression, causes G2/M cell cycle arrest in proliferating cells, and promotes apoptosis via caspase-3 and PARP cleavage. Tirbanibulin has demonstrated potent activity against a range of solid tumors and leukemia cell lines—including those resistant to other cancer drugs—and is approved for topical treatment of actinic keratosis. Paclitaxel is a well-established chemotherapy agent that stabilizes microtubules and prevents their depolymerization during cell division, thereby inhibiting mitosis in cancer cells. The combination of tirbanibulin (KX2-391) with paclitaxel has been studied in clinical trials for oncology indications such as solid tumors[1][2][3][5].

Other names
tirbanibulinTaxol
02

Targets

TUBB (Tubulin (alpha and beta subunits))SRC (Proto-oncogene tyrosine-protein kinase Src)

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