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indinavir

Trade name: crixivan

Small moleculeapproved

Approved

Mar 13, 1996

Indinavir is an antiretroviral drug for the treatment of HIV infection. Indinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Indinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs. — NCATS

Clinical trial activity

100 trials · 41 clinical orgs · 1 marketing orgs

Phase 1
14
Phase 2
50
Phase 3
14
Phase 4
9

Earliest trial started Jul 1, 1995 (NCT00001443)

Timeline

1990s

  1. Jan 1, 1995

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1996

    Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 1996

    Earliest Phase 3 Sponsor(trial)

  4. Mar 13, 1996

    Merck — Earliest FDA Approval

  5. Mar 13, 1996

    Merck — NDA Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedMar 13, 1996

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)(C)NC(=O)[C@@H]1CN(Cc2cccnc2)CCN1C[C@@H](O)C[C@@H](Cc1ccccc1)C(=O)N[C@H]1c2ccccc2C[C@H]1O
Mol. weight
613.8 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Discontinued

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • (1(1s,2r),5(s))-2,3,5-trideoxy-n-(2,3-dihydro-2-hydroxy-1h-inden-1-yl)-5-(2-(((1,1-dimethylethyl)amino)carbonyl)-4-(3-pyridinylmethyl)-1-piperazinyl)-2-(phenylmethyl)-d-erythro-pentonamide
  • (1(1s,2r),5(s))-2,3,5-trideoxy-n-(2,3-dihydro-2-hydroxy-1h-inden-1-yl)-5-(2-(((1,1-dimethylethyl)amino)carbonyl)-4-(3-pyridinylmethyl)-1-piperazinyl)-2-(phenylmethyl)-d-erythro-pentonamide
  • crixivan
  • crixivan
  • crixivan
  • crixivan
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir
  • indinavir anhydrous
  • indinavir anhydrous
  • indinavir sulfate
  • indinavir sulfate
  • indinavir sulfate
  • indinavir sulfate
  • indinavir sulphate
  • indinavir sulphate
  • l-735524
  • l-735524
  • mk0639
  • mk-639
  • mk-639

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02556268Phase 1Feb 1, 2016Bayer
NCT02858401Phase 1Jan 29, 2015Gilead Sciences
NCT01067690Phase 2Jun 1, 2008Bankura Sammilani Medical College, Istituto Superiore di Sanità
NCT00637637Phase 2Sep 1, 2007Ospedale S. Giovanni Bellinzona
NCT00445146Phase 2Feb 1, 2007Gilead Sciences
NCT00411996Phase 1/Phase 2 (Phase 2)Dec 1, 2006HIV-NAT Thai Red Cross AIDS Research Center, The HIV Netherlands Australia Thailand Research Collaboration
NCT00385957Phase 4Oct 10, 2006University of Barcelona
NCT00148785Phase 4Jul 1, 2005Emory University
NCT00307502Phase 1Jan 1, 2005Badalona Hospital Germans Trias i Pujol, Fundacio Lluita Contra la SIDA, University of Barcelona
NCT00232908Phase 4Jun 1, 2004Roche
NCT00362310Phase 2Jun 1, 2003Istituto Superiore di Sanità
NCT00192660Phase 4Feb 1, 2003National Heart, Lung, and Blood Institute (NHLBI), The National Centre in HIV Epidemiology and Clinical Research, Sydney, University of New South Wales
NCT00158405Phase 3Dec 1, 2002Bristol-Myers Squibb, CHU Treichville, French National Agency for Research on AIDS and Viral Hepatitis, Programme PACCI Abidjan
NCT00050180Phase 4Nov 22, 2002National Cancer Institute (NCI), National Institutes of Health (NIH)
NCT00039741Phase 2/Phase 3 (Phase 3)Aug 1, 2002Duke University, National Institute of Allergy and Infectious Diseases (NIAID), National Institutes of Health (NIH), PENTA Foundation, University of Washington
NCT00122590N/AJul 1, 2002French National Agency for Research on AIDS and Viral Hepatitis, Roche, University of Paris
NCT00039975Phase 1Jun 18, 2002National Institute of Allergy and Infectious Diseases (NIAID)
NCT00120783Phase 2Feb 1, 2002French National Agency for Research on AIDS and Viral Hepatitis
NCT00027339Phase 2Dec 4, 2001National Institute of Allergy and Infectious Diseases (NIAID), University of California, San Diego, University of North Carolina at Chapel Hill
NCT00016601N/AJun 1, 2001National Institute of Allergy and Infectious Diseases (NIAID), National Institutes of Health (NIH)
Showing 20 of 100 trials
Page 1 / 5

Organizations

Research & Development (41)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute of Allergy and Infectious Diseases (NIAID)Government393941997
MerckFor profit212151999
Glaxo WellcomeFor profit7731999
National Institutes of Health (NIH)Government6151996
Bristol-Myers SquibbFor profit4321996
National Cancer Institute (NCI)Government4231995
French National Agency for Research on AIDS and Viral HepatitisGovernment3332002
Gilead SciencesFor profit3321999
Pharmacia & UpjohnFor profit3311999
University of BarcelonaAcademic/Hospital3222000
AgouronFor profit2121999
DuPont MerckFor profit2211999
Istituto Superiore di SanitàAcademic/Hospital2212003
RocheFor profit2122002
AbbottFor profit1111999
AIDS Malignancy ConsortiumAcademic/Hospital1011997
Badalona Hospital Germans Trias i PujolAcademic/Hospital1112005
Bankura Sammilani Medical CollegeAcademic/Hospital1012008
BayerFor profit1112016
CHU TreichvilleAcademic/Hospital1012002
41 organizations
Page 1 / 3

Marketing (1)

OrganizationOrg typeRelationshipDate
MerckFor profitNDAMar 13, 1996