etravirine (intelence) Report issue

Small molecule Approved FDA Accelerated Approval FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

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Etravirine (formerly known as TMC125) is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor. Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. In combination with other antiretroviral agents, it is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced adult patients, who have evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) and other antiretroviral agents. The most common adverse events (incidence > 10%) of any intensity that occurred at a higher rate than placebo are rash and nausea. Etravirine should not be co-administered with the following antiretrovirals: Tipranavir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir; Protease inhibitors administered without ritonavir; NNRTIs.   NCATS

Chemistry

  • SMILES: CC1=CC(=CC(C)=C1OC2=C(Br)C(N)=NC(NC3=CC=C(C=C3)C#N)=N2)C#N
  • InChIKey: PYGWGZALEOIKDF-UHFFFAOYSA-N
  • Mol. Mass: 435.277
  • ALogP: 4.72
  • ChEMBL Molecule:
    etravirine  
More Chemistry

Pharmacology

Drug Pricing (per unit)

United States

$2.1288 - $22.8535

Australia

$6.8111
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-benzonitrile | benzonitrile, 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl- | etravirin | etravirine | intelence | r165335 | r-165335 | tmc125 | tmc 125 | tmc-125 | tmc125 cpd

Organizations (42)

Research & Development (40)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (4)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (19)

Approved Indications (2)


 

HIV

HIV Infections

Experimental Indications - Clinical Trial Phases 1-4 (19)


 

Acquired Immunodeficiency Syndrome (Phase 2)

Anti-Retroviral Agents (Phase 2)

Carcinoma, Hepatocellular (Phase 4)

Endothelium (Phase 1)

Friedreich Ataxia (Phase 2)

Healthy Volunteers (Phase 1)

Hepatitis B (Phase 4)

Hepatitis B, Chronic (Phase 4)

Hepatitis C (Phase 1)

Hepatitis C, Chronic (Phase 4)

HIV (Phase 4)

HIV-1 (Phase 3)

HIV Infections ()

Inflammation (Phase 1)

Insulin Resistance (Phase 1)

Lipids (Phase 1)

Mycoses (Phase 1)

Pharmacokinetics (Phase 1)

Pregnancy (Phase 3)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 61
  • # of Trial Organizations: 40

Trials by Phase

Trial Phase Start Date Organizations Indications

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