Drug intelligence / Profile preview

thailanstatin A

Development stage
Preclinical
Lead developer
Peak Bio
Modality
Small Molecules
Administration
Intravenous
01

Overview

Thailanstatin A is a natural product-derived small molecule that serves as a potent cytotoxic payload for antibody-drug conjugates (ADCs). Isolated from the bacterium *Burkholderia thailandensis*, it belongs to the spliceostatin class of compounds and functions as a spliceosome inhibitor. Its primary mechanism involves binding to the SF3b subunit of the U2 small nuclear ribonucleoprotein (snRNP) complex, which disrupts the recognition of the branch point sequence during pre-mRNA splicing. This inhibition leads to defective splicing, cell cycle arrest, and the induction of apoptosis in cancer cells. Shanghai Hisun Pharmaceutical Technology is developing Thailanstatin A as a specialized payload for oncological ADC applications, with the project currently in preclinical manufacturing development stages, including bench-scale and pilot-scale validation.

Other names
Thailanstatin A
02

Targets

SF3B1 (Splicing factor 3B subunit 1)

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