General Information of DTT (ID: TT5FNQT)

DTT Name Human immunodeficiency virus Protease (HIV PR) DTT Info
Gene Name HIV PR

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
8 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amprenavir DMLMXE0 Human immunodeficiency virus infection 1C62 Approved [1]
Atazanavir DMSYRBX Human immunodeficiency virus infection 1C62 Approved [2]
Darunavir DMN3GCH Human immunodeficiency virus infection 1C62 Approved [3]
Fosamprenavir DM4W9B3 Human immunodeficiency virus infection 1C62 Approved [4]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [5]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [6]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [7]
Tipranavir DM8HJX6 Human immunodeficiency virus infection 1C62 Approved [8]
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⏷ Show the Full List of 8 Approved Drug(s)
16 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BI 201335 DM3MXT8 Hepatitis C virus infection 1E51.1 Phase 3 [9]
ABT-450 DMFW860 Hepatitis C virus infection 1E51.1 Phase 2 [10]
ACH-1625 DMIVUFL Hepatitis C virus infection 1E51.1 Phase 2 [11]
BMS 650032 DMQI43G Hepatitis C virus infection 1E51.1 Phase 2 [12]
Danoprevir DM20MDU Hepatitis C virus infection 1E51.1 Phase 2 [13]
DG-17 DMS9Y1T Human immunodeficiency virus infection 1C62 Phase 2 [14]
GS-9256 DMCZH5B Hepatitis C virus infection 1E51.1 Phase 2 [15]
KNI-272 DMQZ5HF Human immunodeficiency virus infection 1C62 Phase 2 [16]
MK-5172 DMSPWX6 Hepatitis C virus infection 1E51.1 Phase 2 [17]
TMC-310911 DMW145U Human immunodeficiency virus infection 1C62 Phase 2 [18]
Vaniprevir DMCF5E0 Hepatitis C virus infection 1E51.1 Phase 2 [17]
BIT225 DMGAR9Y Hepatitis C virus infection 1E51.1 Phase 1 [19]
CTP-298 DMIKX01 Human immunodeficiency virus infection 1C62 Phase 1 [20]
PF-04776548 DMLGD0V Human immunodeficiency virus infection 1C62 Phase 1 [21]
PPL-100 DMOYUPM Human immunodeficiency virus infection 1C62 Phase 1 [22]
VX-500 DM8UTPJ Hepatitis C virus infection 1E51.1 Phase 1 [23]
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⏷ Show the Full List of 16 Clinical Trial Drug(s)
33 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
A-75925 DMF4MRD Virus infection 1A24-1D9Z Discontinued in Phase 2 [24]
BRECANAVIR DMRVH2S Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [25]
MK-944a DMOZUPB Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [26]
Mozenavir DMLG7QB Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [27]
R-87366 DMRZI3C Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [28]
Telinavir DM8OWID Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [29]
GS-9005 DM7R126 Human immunodeficiency virus infection 1C62 Discontinued in Phase 1/2 [30]
A-80987 DMGEWQ7 Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [31]
CGP-53437 DMF0O2H Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [32]
DMP-851 DM412S9 Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [33]
DPC-681 DM5HAG0 Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [34]
DPC-684 DMS19VG Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [34]
KNI-764 DM6LTRC Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [35]
LASINAVIR DMHEKIN Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [36]
R-944 DMJ2ZVW Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [37]
SPI-256 DMKGL2I Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [38]
U-103017 DMTVC3W Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [39]
U-96988 DML73BR Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [40]
XM-323 DMQKH07 Human immunodeficiency virus infection 1C62 Discontinued in Phase 1 [41]
AG-1284 DMRI7YB Human immunodeficiency virus infection 1C62 Terminated [42]
AG-1350 DMALV1W Human immunodeficiency virus infection 1C62 Terminated [43]
BAY-793 DM69EHF Human immunodeficiency virus infection 1C62 Terminated [44]
BMS-182193 DMEDLHG Human immunodeficiency virus infection 1C62 Terminated [45]
BMS-186318 DMKZ3PW Human immunodeficiency virus-1 infection 1C62 Terminated [46]
CGP-70726 DMRLXC3 Human immunodeficiency virus-1 infection 1C62 Terminated [47]
Droxinavir hydrochloride DM6EJVF Human immunodeficiency virus infection 1C62 Terminated [48]
GE-20372A DMGM3VP Human immunodeficiency virus infection 1C62 Terminated [49]
GS-2992 DMPSZR0 Human immunodeficiency virus infection 1C62 Terminated [49]
KNI-102 DMXZNB2 Human immunodeficiency virus infection 1C62 Terminated [50]
Palinavir DMLKQUR Human immunodeficiency virus infection 1C62 Terminated [51]
PD-153103 DMVEXID Human immunodeficiency virus-1 infection 1C62 Terminated [49]
SB-206343 DMYFE23 Human immunodeficiency virus-1 infection 1C62 Terminated [52]
U-75875 DMRBXEA Human immunodeficiency virus infection 1C62 Terminated [53]
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⏷ Show the Full List of 33 Discontinued Drug(s)
2 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
JG-365 DMQP4VG Discovery agent N.A. Investigative [54]
KH-164 DMCE8Q9 Discovery agent N.A. Investigative [55]
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Molecule Interaction Atlas

References

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21 ClinicalTrials.gov (NCT01045317) A Study To Investigate The Clearance Of PF-04776548 From The Body Following A Very Low (Micro) Dose Of The Compound Using A Low Level Of Radiotracer To Help Quantify Expected Low Concentrations Of PF-04776548 In The Body. U.S. National Institutes of Health.
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24 Solvation studies of DMP323 and A76928 bound to HIV protease: analysis of water sites using grand canonical Monte Carlo simulations. Protein Sci. 1998 Mar;7(3):573-9.
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26 Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. J Med Chem. 2000 Sep 7;43(18):3386-99.
27 Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450. Chem Biol. 1996 Apr;3(4):301-14.
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29 Improvement of bioavailability of the HIV protease inhibitor SC-52151 in the beagle dog by coadministration of the CYP3A4 inhibitor, ketoconazole. Xenobiotica. 1997 May;27(5):489-97.
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38 Current and Novel Inhibitors of HIV Protease. Viruses. 2009 December; 1(3): 1209-1239.
39 Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. J Med Chem. 1995 Dec 22;38(26):4968-71.
40 Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. J Med Chem. 1994 Sep 30;37(20):3200-4.
41 In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor. Antimicrob Agents Chemother. 1993 Dec;37(12):2606-11.
42 Exploring the energy landscapes of molecular recognition by a genetic algorithm: analysis of the requirements for robust docking of HIV-1 protease and FKBP-12 complexes. Proteins. 1996 Jul;25(3):342-53.
43 Ly316340: A potent HIV-1 protease inhibitor containing a high affinity octahydrothienopyridine hydroxyethylamine isostere. Bioorganic & Medicinal Chemistry Letters Volume 5, Issue 23, 7 December 1995, Pages 2885-2890.
44 HIV protease inhibitor HOE/BAY 793, structure-activity relationships in a series of C2-symmetric diols. Bioorg Med Chem. 1995 May;3(5):559-71.
45 Antiviral properties of aminodiol inhibitors against human immunodeficiency virus and protease. Antimicrob Agents Chemother. 1995 Feb;39(2):374-9.
46 Determination of BMS-186318 in dog, rat and monkey plasma by liquid chromatography-ionspray mass spectrometry. J Pharm Biomed Anal. 1995 Dec;14(1-2):43-8.
47 Oral bioavailability of a poorly water soluble HIV-1 protease inhibitor incorporated into pH-sensitive particles: effect of the particle size and nutritional state. J Control Release. 2000 Aug 10;68(2):291-8.
48 A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A. Antimicrob Agents Chemother. 1997 Mar;41(3):515-22.
49 US patent application no. 2008,0161,324, Compositions and methods for treatment of viral diseases.
50 KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic. Chem Pharm Bull (Tokyo). 1991 Nov;39(11):3088-90.
51 Antiviral properties of palinavir, a potent inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1997 May;41(5):965-71.
52 Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere. J Med Chem. 1994 Sep 16;37(19):3100-7.
53 Effects of U-75875, a peptidomimetic inhibitor of retroviral proteases, on simian immunodeficiency virus infection in rhesus monkeys. Antimicrob Agents Chemother. 1994 Jun;38(6):1277-83.
54 [Mechanism of action of aspartic proteases. III. Conformational characteristics of HIV-1 protease inhibitor JG-365]. Bioorg Khim. 1999 Jun;25(6):418-22.
55 Impeded progression of Friend disease in mice by an inhibitor of retroviral proteases. J Acquir Immune Defic Syndr. 1993 Jan;6(1):24-31.