Drug intelligence / Profile preview

phenformin

Development stage
Phase 2
Lead developer
U.S. Vitamin Corporation
Modality
Small Molecules
Administration
Oral
01

Overview

Phenformin is an oral antidiabetic drug of the biguanide class, formerly used to treat type 2 diabetes mellitus. It lowers blood glucose by decreasing hepatic gluconeogenesis, delaying intestinal glucose absorption, and increasing insulin sensitivity in peripheral tissues. Its primary mechanism involves activation of AMP‑activated protein kinase (AMPK), leading to improved glycemic control. Unlike sulfonylureas, it does not stimulate insulin secretion but requires endogenous insulin for its hypoglycemic effect. Due to a high risk of lactic acidosis—often fatal—phenformin was withdrawn from most markets in the late 1970s and replaced by metformin, which has a better safety profile[1][2][4][5][6]. Research has also explored phenformin’s potential anticancer effects via inhibition of mitochondrial complex I and mTOR signaling[2].

Brand names
DBIMeltrolDiparCronoforminFenfoduronFenorminGlukopostinPhenformixDebeoneDiabisDibirafDibotinGlyphenRetardoDb-retardFeguanideLentobeticNormoglucinaAzucapsDebinylDibeinInsoralDB Comb
Other names
PhenformineFenforminFenforminaPhenethyldiguanidePhenylethylbiguanideImidodicarbonimidic diamide, N-(2‑phenylethyl)-beta‑PEBG1‑Phenethylbiguanidebeta‑PhenethylbiguanidePhenforminum
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)KCNJ8 (ATP-sensitive potassium channel subunit Kir6.1)

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