Drug intelligence / Profile preview

syrosingopine

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intraperitoneal (research Use, Animal Studies)
01

Overview

**Syrosingopine** is a synthetic antihypertensive agent, originally introduced around 1960 and chemically derived from reserpine. It is the methyl reserpate ester of syringic acid ethyl carbonate. Syrosingopine acts as a **dual inhibitor of the lactate transporters MCT1 and MCT4**, leading to increased intracellular lactate and inhibition of glycolysis. It also depletes peripheral neuronal noradrenaline stores, accounting for its antihypertensive and monoamine-depleting effects. More recently, it has been studied for its anti-cancer properties, particularly its ability to induce synthetic lethality in combination with mitochondrial inhibitors such as metformin by disrupting tumor metabolism. It is orally active and has a history of over 40 years’ use as an antihypertensive, though currently it is mainly used in research as it is not a marketed antihypertensive anymore.

Brand names
Singoserp
Other names
syrosingopine
02

Targets

ENO (Alpha-enolase)VMAT2 (Vesicular monoamine transporter 2)MCT4 (Monocarboxylate transporter 4)SLC16A1 (Mitochondrial Pyruvate Carrier)

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