Epristeride
Encyclopedia
Epristeride is a selective
, transition state, non-competitive inhibitor
of the type II isoform of the enzyme
5α-reductase, similarly to finasteride
and turosteride
. It was under development for the treatment of benign prostatic hyperplasia
(BPH) and acne vulgaris
by SmithKline Beecham (now GlaxoSmithKline
), and reached phase III clinical trial
s in the United States
, United Kingdom
, and Japan
, but ultimately was never marketed.
Binding selectivity
Binding selectivity refers to the differing affinities with which different ligands bind to a substrate forming a complex. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate...
, transition state, non-competitive inhibitor
Enzyme inhibitor
An enzyme inhibitor is a molecule that binds to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used as herbicides and pesticides...
of the type II isoform of the enzyme
Enzyme
Enzymes are proteins that catalyze chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical reactions in a biological cell need enzymes in order to occur at rates...
5α-reductase, similarly to finasteride
Finasteride
Finasteride is a synthetic antiandrogen that inhibits type II 5-alpha reductase, the enzyme that converts testosterone to dihydrotestosterone...
and turosteride
Turosteride
Turosteride is a selective inhibitor of the enzyme 5α-redcutase which was under investigation by GlaxoSmithKline for the treatment of benign prostatic hyperplasia , but was never marketed. Similarly to finasteride, turosteride is selective for the type II isoform of 5α-redcutase, with about...
. It was under development for the treatment of benign prostatic hyperplasia
Benign prostatic hyperplasia
Benign prostatic hyperplasia also known as benign prostatic hypertrophy , benign enlargement of the prostate , and adenofibromyomatous hyperplasia, refers to the increase in size of the prostate....
(BPH) and acne vulgaris
Acne vulgaris
Acne vulgaris is a common human skin disease, characterized by areas of skin with seborrhea , comedones , papules , pustules , Nodules and possibly scarring...
by SmithKline Beecham (now GlaxoSmithKline
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
), and reached phase III clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
, United Kingdom
United Kingdom
The United Kingdom of Great Britain and Northern IrelandIn the United Kingdom and Dependencies, other languages have been officially recognised as legitimate autochthonous languages under the European Charter for Regional or Minority Languages...
, and Japan
Japan
Japan is an island nation in East Asia. Located in the Pacific Ocean, it lies to the east of the Sea of Japan, China, North Korea, South Korea and Russia, stretching from the Sea of Okhotsk in the north to the East China Sea and Taiwan in the south...
, but ultimately was never marketed.