Drug intelligence / Profile preview

TAK-495

Development stage
Discontinued
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

TAK-495 is a small molecule antagonist of the **Smoothened (SMO) receptor**, a key component of the **Hedgehog (Hh) signaling pathway**. Developed by **Takeda Pharmaceuticals**, TAK-495 was designed to inhibit the aberrant activation of the Hh pathway, which is a known driver in several malignancies, including **basal cell carcinoma** and **medulloblastoma**. By binding to the SMO receptor, TAK-495 prevents the downstream signaling cascade that leads to the activation of GLI transcription factors, thereby suppressing the expression of genes involved in tumor cell proliferation, survival, and epithelial-mesenchymal transition. Although it demonstrated potent preclinical activity, TAK-495 was primarily a backup or follow-up compound to TAK-441 and its clinical development was ultimately discontinued.

02

Targets

HCRTR1 (Orexin/hypocretin receptor type 1)

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