TAS-108

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DB05966InvestigationalSmall molecule

Investigated for use/treatment in breast cancer.

Mechanism: TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues. In addition, TAS-108 activates the co-repressor Silencing Mediator for Retinoid and Thyroid hormone receptor (SMRT), a protein that inhibits the activities of the estrogen receptors, which may contribute to the antitumor activity of TAS-108.
Curator reviewed
Primary indication: Investigated for use/treatment in breast cancer.Curator reviewed
Formula / weight: C₃₉H₅₅NO₁₀ · 697.866 g/mol (avg)
Code names: TAS-108

Resolves to

Compound

UNII9B29N23K7ECAS229634-97-3

Structure

InChIKeyVOHOCSJONOJOSD-SCIDSJFVSA-NSMILESOC(=O)CC(O)(CC(O)=O)C(O)=O.CCN(CC)CC1=CC=C(OCC[C@H]2CC[C@H]3[C@@H]4[C@H](C)CC5=C(C=CC(O)=C5)[C@H]4CC[C@]23C)C(OC)=C1

Targets

P03372ESR1Q92731ESR2

What you can answer from here — as of June 15, 2026

2Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

1Clinical trialPhase, status and sponsor resolved per trial

4+ReferencesStructured and connected to the statements they support

Which drugs share a target with TAS-108, and which of those have an active Phase 3 trial?

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