Delving into the Latest Updates on Org-33201 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

aromatase

Mechanism

aromatase inhibitors(Aromatase inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Breast Cancer

Originator Organization

MSD Oss BV

Active Organization-

Inactive Organization

MSD Oss BV

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

Org 33201 has been selected as a very potent aromatase inhibitor. The compound is an enantiomer of a SC2H5 substituted imidazoylethylphenalene. Org 33201 inhibited human aromatase activity for 50% at a concentration of 2.2 x 10(9) mol/l. More than 200-fold higher concentrations were needed for the inhibition of other cytochrome P-450 enzymes. In vivo the compound was active in rats (ED50 = 0.035 mg/kg) and dogs (1 mg/kg gave 70% inhibition) after oral administration. It can be concluded that Org 33201 is a potent and highly selective orally active aromatase inhibitor.

100 Deals associated with Org-33201

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