Drug intelligence / Profile preview

azd3409

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

Overview

AZD3409 is an orally active small molecule antitumor agent developed as a double prodrug that acts as a dual prenyltransferase inhibitor. It inhibits both farnesyl transferase (FTase) and geranylgeranyl transferase 1 (GGTase-1), with modest selectivity for FTase. The drug is metabolized in plasma and cells to its active acid form via esterases. By inhibiting protein farnesylation—particularly of Ras proteins—AZD3409 disrupts the Ras signal transduction pathway involved in tumor growth and survival. Preclinical studies demonstrated significant antitumor activity in various cancer models. Clinical development included phase I trials for solid tumors and hepatitis D; however, further development was discontinued[1][2][3][4][5][6][7].

Other names
345915-10-8UNII-F99W9H5WUEUNII-F-99W9H5WUEUNII-F 99W9H5WUEF99W9H5WUEF-99W9H5WUEF 99W9H5WUE
02

Targets

GGTase I (Geranylgeranyl transferase type I)FTase (Protein Farnesyltransferase)

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