Drug intelligence / Profile preview

azd3965

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZD3965 is an orally available small molecule inhibitor of monocarboxylate transporter 1 (MCT1), developed for its potential antineoplastic activity. By selectively binding to MCT1 on tumor cells—which is responsible for the transport of lactate and other monocarboxylates across the cell membrane—AZD3965 blocks lactate influx and efflux. This inhibition leads to intracellular accumulation of lactate and acidification within cancer cells, disrupting their metabolism and resulting in cell death. The drug shows selectivity for MCT1 over other related transporters such as MCT2, MCT3, and MCT4. It has demonstrated preclinical efficacy particularly in hematological malignancies like lymphoma[1][2][6].

Other names
(S)-5-(4-Hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione1448671-31-5
02

Targets

MCT2 (Monocarboxylate transporter 2)SLC16A1 (Mitochondrial Pyruvate Carrier)

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