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  • Protease Inhibitor (Pharmacology) : Protease Inhibitors (Pis) Are A Class of Drugs Used To Treat or Prevent

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    Protease inhibitor (pharmacology) From Wikipedia, the free encyclopedia Jump to: navigation, search For natural protease inhibitors, see protease inhibitor (biology). Protease inhibitors (PIs) are a class of drugs used to treat or prevent infection by viruses, including HIV and Hepatitis C. PIs prevent viral replication by inhibiting the activity of proteases, e.g. HIV-1 protease, enzymes used by the viruses to cleave nascent proteins for final assembly of new virions. Protease inhibitors have been developed or are presently undergoing testing for treating various viruses: • HIV/AIDS: antiretroviral protease inhibitors (saquinavir, ritonavir, indinavir, nelfinavir, amprenavir[1] etc.) • Hepatitis C: Boceprevir • Hepatitis C: Telaprevir Given the specificity of the target of these drugs there is the risk, as in antibiotics, of the development of drug-resistant mutated viruses. To reduce this risk it is common to use several different drugs together that are each aimed at different targets. Contents • 1 Antiretrovirals • 2 Antiprotozoal Activity • 3 Anticancer Activity • 4 Side Effects • 5 See also • 6 References • 7 External links Antiretrovirals Protease inhibitors were the second class of antiretroviral drugs developed. In all cases, patents remain in force until 2010 or beyond. Name Trade name Company Patent Notes Saquinavir Fortovase, Invirase Hoffmann–La Roche U.S. Patent 5,196,438 It was the first protease inhibitor approved by the FDA (December 6, 1995). Ritonavir Norvir Abbott Laboratories U.S. Patent 5,541,206 - Indinavir Crixivan Merck & Co. U.S. Patent 5,413,999 - Nelfinavir Viracept Agouron Pharmaceuticals U.S. Patent 5,484,926 - Amprenavir Agenerase GlaxoSmithKline U.S. Patent 5,585,397 The FDA approved it April 15, 1999, making it the sixteenth FDA-approved antiretroviral. It was the first protease inhibitor approved for twice-a-day dosing instead of needing to be taken every eight hours. The convenient dosing came at a price, as the dose required is 1,200 mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir. Lopinavir Kaletra Abbott - Is only marketed as a combination, with ritonavir. Atazanavir Reyataz Bristol-Myers Squibb - The FDA approved it on June 20, 2003. Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs. Fosamprenavir Lexiva, Telzir GlaxoSmithKline - Is a prodrug of amprenavir. The FDA approved it October 20, 2003. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a slow-release version of amprenavir and thus reduces the number of pills required versus standard amprenavir. Tipranavir Aptivus Boehringer-Ingelheim - Also known as tipranavir disodium Darunavir Prezista Tibotec - It was approved by the Food and Drug Administration (FDA) on June 23, 2006. Prezista is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents.[2] Several ongoing phase III trials are showing a high efficiency for the PREZISTA/rtv combination being superior to the lopinavir/rtv combination for first-line therapy.[3] Darunavir is the first drug in a long time that didn't come with a price increase. It leapfrogged two other approved drugs of its type, and is matching the price of a third.[4][5][6] Antiprotozoal Activity Researchers are investigating the use of protease inhibitors developed for HIV treatment as anti-protozoals for use against malaria and gastrointestinal protozoal infections: • A combination of ritonavir and lopinavir was found to have some effectiveness against Giardia infection.[7] • The drugs saquinavi

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    Protease inhibitor (pharmacology) From Wikipedia, the free encyclopedia Jump to: navigation, search For natural protease inhibitors, see protease inhibitor (biology). Protease inhibitors (PIs) are a class of drugs used to treat or prevent infection by viruses, including HIV and Hepatitis C. PIs prevent viral replication by inhibiting the activity of proteases, e.g. HIV-1 protease, enzymes used by the viruses to cleave nascent proteins for final assembly of new virions. Protease inhibitors have been developed or are presently undergoing testing for treating various viruses: • HIV/AIDS: antiretroviral protease inhibitors (saquinavir, ritonavir, indinavir, nelfinavir, amprenavir[1] etc.) • Hepatitis C: Boceprevir • Hepatitis C: Telaprevir Given the specificity of the target of these drugs there is the risk, as in antibiotics, of the development of drug-resistant mutated viruses. To reduce this risk it is common to use several different drugs together that are each aimed at different targets. Contents • 1 Antiretrovirals • 2 Antiprotozoal Activity • 3 Anticancer Activity • 4 Side Effects • 5 See also • 6 References • 7 External links Antiretrovirals Protease inhibitors were the second class of antiretroviral drugs developed. In all cases, patents remain in force until 2010 or beyond. Name Trade name Company Patent Notes Saquinavir Fortovase, Invirase Hoffmann–La Roche U.S. Patent 5,196,438 It was the first protease inhibitor approved by the FDA (December 6, 1995). Ritonavir Norvir Abbott Laboratories U.S. Patent 5,541,206 - Indinavir Crixivan Merck & Co. U.S. Patent 5,413,999 - Nelfinavir Viracept Agouron Pharmaceuticals U.S. Patent 5,484,926 - Amprenavir Agenerase GlaxoSmithKline U.S. Patent 5,585,397 The FDA approved it April 15, 1999, making it the sixteenth FDA-approved antiretroviral. It was the first protease inhibitor approved for twice-a-day dosing instead of needing to be taken every eight hours. The convenient dosing came at a price, as the dose required is 1,200 mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir. Lopinavir Kaletra Abbott - Is only marketed as a combination, with ritonavir. Atazanavir Reyataz Bristol-Myers Squibb - The FDA approved it on June 20, 2003. Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs. Fosamprenavir Lexiva, Telzir GlaxoSmithKline - Is a prodrug of amprenavir. The FDA approved it October 20, 2003. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a slow-release version of amprenavir and thus reduces the number of pills required versus standard amprenavir. Tipranavir Aptivus Boehringer-Ingelheim - Also known as tipranavir disodium Darunavir Prezista Tibotec - It was approved by the Food and Drug Administration (FDA) on June 23, 2006. Prezista is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents.[2] Several ongoing phase III trials are showing a high efficiency for the PREZISTA/rtv combination being superior to the lopinavir/rtv combination for first-line therapy.[3] Darunavir is the first drug in a long time that didn't come with a price increase. It leapfrogged two other approved drugs of its type, and is matching the price of a third.[4][5][6] Antiprotozoal Activity Researchers are investigating the use of protease inhibitors developed for HIV treatment as anti-protozoals for use against malaria and gastrointestinal protozoal infections: • A combination of ritonavir and lopinavir was found to have some effectiveness against Giardia infection.[7] • The drugs saquinavi

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    Protease Inhibitor (Pharmacology) : Protease Inhibitors (Pis) Are A Class of Drugs Used To Treat or Prevent

    Загружено:

    Else
    Protease inhibitor (pharmacology) From Wikipedia, the free encyclopedia Jump to: navigation, search For natural protease inhibitors, see protease inhibitor (biology). Protease inhibitors (PIs) are a class of drugs used to treat or prevent infection by viruses, including HIV and Hepatitis C. PIs prevent viral replication by inhibiting the activity of proteases, e.g. HIV-1 protease, enzymes used by the viruses to cleave nascent proteins for final assembly of new virions. Protease inhibitors have been developed or are presently undergoing testing for treating various viruses: • HIV/AIDS: antiretroviral protease inhibitors (saquinavir, ritonavir, indinavir, nelfinavir, amprenavir[1] etc.) • Hepatitis C: Boceprevir • Hepatitis C: Telaprevir Given the specificity of the target of these drugs there is the risk, as in antibiotics, of the development of drug-resistant mutated viruses. To reduce this risk it is common to use several different drugs together that are each aimed at different targets. Contents • 1 Antiretrovirals • 2 Antiprotozoal Activity • 3 Anticancer Activity • 4 Side Effects • 5 See also • 6 References • 7 External links Antiretrovirals Protease inhibitors were the second class of antiretroviral drugs developed. In all cases, patents remain in force until 2010 or beyond. Name Trade name Company Patent Notes Saquinavir Fortovase, Invirase Hoffmann–La Roche U.S. Patent 5,196,438 It was the first protease inhibitor approved by the FDA (December 6, 1995). Ritonavir Norvir Abbott Laboratories U.S. Patent 5,541,206 - Indinavir Crixivan Merck & Co. U.S. Patent 5,413,999 - Nelfinavir Viracept Agouron Pharmaceuticals U.S. Patent 5,484,926 - Amprenavir Agenerase GlaxoSmithKline U.S. Patent 5,585,397 The FDA approved it April 15, 1999, making it the sixteenth FDA-approved antiretroviral. It was the first protease inhibitor approved for twice-a-day dosing instead of needing to be taken every eight hours. The convenient dosing came at a price, as the dose required is 1,200 mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir. Lopinavir Kaletra Abbott - Is only marketed as a combination, with ritonavir. Atazanavir Reyataz Bristol-Myers Squibb - The FDA approved it on June 20, 2003. Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs. Fosamprenavir Lexiva, Telzir GlaxoSmithKline - Is a prodrug of amprenavir. The FDA approved it October 20, 2003. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a slow-release version of amprenavir and thus reduces the number of pills required versus standard amprenavir. Tipranavir Aptivus Boehringer-Ingelheim - Also known as tipranavir disodium Darunavir Prezista Tibotec - It was approved by the Food and Drug Administration (FDA) on June 23, 2006. Prezista is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents.[2] Several ongoing phase III trials are showing a high efficiency for the PREZISTA/rtv combination being superior to the lopinavir/rtv combination for first-line therapy.[3] Darunavir is the first drug in a long time that didn't come with a price increase. It leapfrogged two other approved drugs of its type, and is matching the price of a third.[4][5][6] Antiprotozoal Activity Researchers are investigating the use of protease inhibitors developed for HIV treatment as anti-protozoals for use against malaria and gastrointestinal protozoal infections: • A combination of ritonavir and lopinavir was found to have some effectiveness against Giardia infection.[7] • The drugs saquinavi

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    © All Rights Reserved
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    Protease inhibitor (pharmacology)

    From Wikipedia, the free encyclopedia


    Jump to: navigation, search
    For natural protease inhibitors, see protease inhibitor (biology).
    Protease inhibitors (PIs) are a class of drugs used to treat or prevent infection by viruses,
    including HIV and Hepatitis C. PIs prevent viral replication by inhibiting the activity of
    proteases, e.g. HIV-1 protease, enzymes used by the viruses to cleave nascent proteins for
    final assembly of new virions.
    Protease inhibitors have been developed or are presently undergoing testing for treating
    various viruses:

    HIV/AIDS: antiretroviral protease inhibitors (saquinavir, ritonavir, indinavir,


    nelfinavir, amprenavir[1] etc.)

    Hepatitis C: Boceprevir

    Hepatitis C: Telaprevir

    Given the specificity of the target of these drugs there is the risk, as in antibiotics, of the
    development of drug-resistant mutated viruses. To reduce this risk it is common to use several
    different drugs together that are each aimed at different targets.

    Contents

    1 Antiretrovirals

    2 Antiprotozoal Activity

    3 Anticancer Activity

    4 Side Effects

    5 See also

    6 References

    7 External links

    Antiretrovirals

    Protease inhibitors were the second class of antiretroviral drugs developed. In all cases,
    patents remain in force until 2010 or beyond.
    Name

    Trade
    name

    Saquinavir

    Fortovase, HoffmannLa
    Invirase Roche

    It was the first protease inhibitor


    approved by the FDA (December 6,
    1995).

    Ritonavir

    Norvir

    Indinavir

    Crixivan

    Nelfinavir

    Viracept

    Company

    Patent

    U.S.
    Patent
    5,196,438
    U.S.
    Abbott
    Patent
    Laboratories
    5,541,206
    U.S.
    Merck & Co.
    Patent
    5,413,999
    U.S.
    Agouron
    Patent
    Pharmaceuticals
    5,484,926

    Notes

    The FDA approved it April 15,


    1999, making it the sixteenth FDAapproved antiretroviral. It was the
    first protease inhibitor approved for
    twice-a-day dosing instead of
    U.S.
    needing to be taken every eight
    Amprenavir Agenerase GlaxoSmithKline Patent
    hours. The convenient dosing came
    5,585,397 at a price, as the dose required is
    1,200 mg, delivered in eight very
    large gel capsules. Production was
    discontinued by the manufacturer
    December 31, 2004, as it has been
    superseded by fosamprenavir.
    Is only marketed as a combination,
    Lopinavir
    Kaletra
    Abbott
    with ritonavir.
    The FDA approved it on June 20,
    2003. Atazanavir was the first PI
    approved for once-daily dosing. It
    Bristol-Myers
    appears to be less likely to cause
    Atazanavir
    Reyataz
    Squibb
    lipodystrophy and elevated
    cholesterol as side effects. It may
    also not be cross-resistant with
    other PIs.
    Fosamprenavir Lexiva,
    GlaxoSmithKline Is a prodrug of amprenavir. The
    Telzir
    FDA approved it October 20, 2003.
    The human body metabolizes
    fosamprenavir in order to form
    amprenavir, which is the active
    ingredient. That metabolization
    increases the duration that
    amprenavir is available, making
    fosamprenavir a slow-release

    version of amprenavir and thus


    reduces the number of pills required
    versus standard amprenavir.
    Tipranavir

    Darunavir

    Aptivus

    Prezista

    BoehringerIngelheim

    Tibotec

    Also known as tipranavir disodium

    It was approved by the Food and


    Drug Administration (FDA) on June
    23, 2006. Prezista is an OARAC
    recommended treatment option for
    treatment-nave and treatmentexperienced adults and adolescents.
    [2]
    Several ongoing phase III trials
    are showing a high efficiency for
    the PREZISTA/rtv combination
    being superior to the lopinavir/rtv
    combination for first-line therapy.[3]
    Darunavir is the first drug in a long
    time that didn't come with a price
    increase. It leapfrogged two other
    approved drugs of its type, and is
    matching the price of a third.[4][5][6]

    Antiprotozoal Activity
    Researchers are investigating the use of protease inhibitors developed for HIV treatment as
    anti-protozoals for use against malaria and gastrointestinal protozoal infections:

    A combination of ritonavir and lopinavir was found to have some effectiveness


    against Giardia infection.[7]

    The drugs saquinavir, ritonavir, and lopinavir have been found to have anti-malarial
    properties.[8]

    A cysteine protease inhibitor drug was found to cure Chagas disease in mice.[9]

    Anticancer Activity
    Researchers are investigating whether protease inhibitors could possibly be used to treat
    cancer. For example, nelfinavir and atazanavir are able to kill tumor cells in culture (in a Petri
    dish).[10][11] This effect has not yet been examined in humans; but studies in laboratory mice
    have shown that nelfinavir is able to suppress the growth of tumors in these animals, which
    represents a promising lead towards testing this drug in humans as well.[11]
    Inhibitors of the proteasome, such as Velcade/Bortezomib are now front-line drugs for the
    treatment of various cancers, notably Multiple Myeloma.

    Side Effects

    Protease inhibitors can cause a syndrome of lipodystrophy, hyperlipidaemia, diabetes mellitus


    type 2, and kidney stones.[12]

    See also

    David Ho - AIDS researcher who pioneered the use of protease inhibitors in treating
    HIV-infected patients

    The Proteolysis Map

    Reverse transcriptase inhibitor

    References
    1.

    ^ Rang, H. P., Dale, M. M., Ritter, J. M., & Flower, R. J. (2007). Rang and
    Dale's Pharmacology (6th Edition ed.). Philadelphia: Churchill Livingstone Elsevier.

    2.

    ^ Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults


    and Adolescents, November 3, 2008, Developed by the DHHS Panel on Antiretroviral
    Guidelines for Adults and Adolescents A Working Group of the Office of AIDS
    Research Advisory Council (OARAC). full guidelines.

    3.

    ^ Madruga JV, Berger D, McMurchie M et al (Jul 2007). "Efficacy and safety


    of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in
    treatment-experienced, HIV-infected patients in TITAN: a randomised controlled
    phase III trial". Lancet 370 (9581): 4958. doi:10.1016/S0140-6736(07)61049-6.
    PMID 17617272.

    4.

    ^ Liz Highleyman, Patient Advocates Commend Pricing of New PI Darunavir,


    http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html

    5.

    ^ [Darunavir - first molecule to treat drug-resistant HIV, http://www.newsmedical.net/?id=19211]

    6.

    ^ Borman S (2006). "Retaining Efficacy Against Evasive HIV: Darunavir


    analog to AIDS-virus shapeshifters: Resistance may be futile". Chemical &
    Engineering News 84 (34): 9.

    7.

    ^ Dunn LA, Andrews KT, McCarthy JS et al (2007). "The activity of protease


    inhibitors against Giardia duodenalis and metronidazole-resistant Trichomonas
    vaginalis". Int. J. Antimicrob. Agents 29 (1): 98102.
    doi:10.1016/j.ijantimicag.2006.08.026. PMID 17137752.

    8.

    ^ Andrews KT, Fairlie DP, Madala PK et al (2006). "Potencies of Human


    Immunodeficiency Virus Protease Inhibitors In Vitro against Plasmodium falciparum
    and In Vivo against Murine Malaria". Antimicrob. Agents Chemother. 50 (2): 63948.
    doi:10.1128/AAC.50.2.639-648.2006. PMC 1366900. PMID 16436721.

    9.

    ^ Doyle PS, Zhou YM, Engel JC, McKerrow JH (2007). "A Cysteine Protease
    Inhibitor Cures Chagas' Disease in an Immunodeficient-Mouse Model of Infection".
    Antimicrobial Agents and Chemotherapy 51 (11): 39329. doi:10.1128/AAC.0043607. PMC 2151429. PMID 17698625.

    10.

    ^ J.J. Gills et al (2007). "Nelfinavir, A Lead HIV Protease Inhibitor, Is a


    Broad-Spectrum, Anticancer Agent that Induces Endoplasmic Reticulum Stress,
    Autophagy, and Apoptosis In vitro and In vivo". Clinical Cancer Research 13 (17):
    518394. doi:10.1158/1078-0432.CCR-07-0161. PMID 17785575.

    11.

    ^ a b Pyrko, P.; Kardosh, A; Wang, W; Xiong, W; Schnthal, AH; Chen, TC


    (2007). "HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma
    death by triggering endoplasmic reticulum stress". Cancer Research 67 (22): 10920
    8. doi:10.1158/0008-5472.CAN-07-0796. PMID 18006837.

    12.

    ^ Protease Inhibitor-Associated Diabetes Mellitus: A Potential Cause of


    Morbidity and Mortality Lori E. Fantry Authors and Disclosures Posted: 03/24/2003;
    J Acquir Immune Defic Syndr. 2003;32(3) 2003 Lippincott Williams & Wilkins

    External links

    A brief history of the development of protease inhibitors by Hoffman La Roche,


    Abbott, and Merck
    [hide]

    Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)

    Entry/fusion
    inhibitors
    (Discovery &
    development)

    Reversetranscriptase
    inhibitors (RTIs)

    gp41 (Enfuvirtide)

    CCR5 (Maraviroc

    Vicriviroc, Cenicriviroc, PRO 140)

    CD4 (Ibalizumab)

    Nucleoside &
    Nucleotide (NRTI)

    Nucleoside analogues/NARTIs:
    Abacavir (ABC)#

    Non-Nucleoside
    (NNRTI)
    (Discovery &
    development)

    Emtricitabine (FTC)#

    Lamivudine (3TC)#

    Didanosine (ddI)#

    Zidovudine (AZT)#

    Apricitabine

    Stampidine

    Elvucitabine

    Racivir

    Amdoxovir

    Stavudine (d4T)#

    Zalcitabine (ddC)

    Festinavir

    Nucleotide analogues/NtRTIs:
    Tenofovir#

    GS 7340

    (1st generation) Efavirenz#

    Nevirapine#

    Loviride

    Delavirdine

    (2nd generation) diarylpyrimidines


    (Etravirine

    Rilpivirine)

    Lersivirine

    Raltegravir

    Elvitegravir

    Dolutegravir

    Globoidnan A (experimental)

    MK-2048

    BI 224436

    Bevirimat

    Vivecon

    Integrase inhibitors

    Maturation
    inhibitors

    1st generation
    Protease Inhibitors
    (PI)
    (Discovery and
    development)

    Fosamprenavir

    Lopinavir#

    Nelfinavir#

    Ritonavir#

    Saquinavir#

    Amprenavir

    Indinavir#

    Atazanavir

    Darunavir

    2nd generation

    Combined
    formulations

    Tipranavir

    Lamivudine/zidovudine

    Emtricitabine/tenofovir/efavirenz

    Abacavir/lamivudine/zidovudine

    Tenofovir/emtricitabine

    Lopinavir/ritonavir

    Abacavir/lamivudine

    Emtricitabine/rilpivirine/tenofovir

    Experimental agents
    Uncoating inhibitors

    TRIM5alpha (gene)

    Transcription
    inhibitors

    Tat antagonists

    Translation inhibitors

    Trichosanthin

    Abzyme

    Calanolide A

    Ceragenin

    Cyanovirin-N

    Diarylpyrimidines

    Epigallocatechin gallate (EGCG)

    Foscarnet

    Other

    Failed agents

    Clinical trials:

    WHO-EM
    Withdrawn from market

    Griffithsin

    Hydroxycarbamide

    Miltefosine

    Portmanteau inhibitors

    Seliciclib

    Synergistic enhancers

    Tre recombinase

    Zinc finger protein transcription


    factor

    KP-1461

    Cobicistat

    Dexelvucitabine

    Capravirine

    Emivirine

    Lodenosine

    Atevirdine

    Brecanavir

    Aplaviroc

    Phase III
    Never to phase III

    DHHS preferred first-line agent. Formerly or rarely used agent.


    M: VIR
    [hide]

    DNA virus antivirals (primarily J05, also S01AD and D06BB)

    Purine
    analogue

    Baltimore I

    TK
    DNA- activate
    d
    synthes
    Herpesvir
    is
    us
    inhibito
    r

    Not TK
    activate
    d

    Pyrimidi
    ne
    analogue

    guanine
    (Aciclovir#/Valacyclovir

    Ganciclovir/Valganciclovir

    Penciclovir/Famciclovir)

    adenine (Vidarabine)

    uridine (Idoxuridine

    Trifluridine

    Edoxudine)

    thymine (Brivudine)

    cytosine (Cytarabine)

    Foscarnet

    Other

    Docosanol

    early protein (Fomivirsen)

    Tromantadine

    Imiquimod/Resiquimod

    Podophyllotoxin

    Vaccinia

    assembly: Rifampicin

    Poxviridae

    Methisazone

    HPV/MC

    Hepatitis B
    (VII)

    Nucleoside analogues/NARTIs: Entecavir

    Lamivudine

    Telbivudine

    Clevudine

    Nucleotide analogues/NtRTIs: Adefovir

    Tenofovir

    Nucleic acid inhibitors

    Multiple/gener
    al

    Cidofovir

    Interferon alfa-2b

    Peginterferon alfa-2a

    Interferon

    Ribavirin#/Taribavirin

    Moroxydine

    Multiple/unknown

    Clinical trials:

    WHO-EM
    Withdrawn from market

    Phase III
    Never to phase III
    M: VIR
    [hide]

    Pharmacology: enzyme inhibition


    Class
    Substrat
    e

    Competitive inhibition Uncompetitive inhibition Non-competitive inhibition


    Suicide inhibition Mixed inhibition
    1.1 Aldose reductase HMG-CoA reductase
    1.3 5-alpha-reductase
    1.4 Monoamine oxidase
    Oxidoreductase
    (EC 1)
    1.5 Dihydrofolate reductase
    1.13 Lipoxygenase
    1.14 Aromatase COX-2
    1.17 Xanthine oxidase Ribonucleotide reductase

    2.1 COMT Thymidylate synthase


    2.4 PARP
    Transferase (EC
    2.5 Dihydropteroate synthetase Farnesyltransferase
    2)
    2.6 GABA transaminase
    2.7 Nucleotidyltransferase (Integrase, Reverse transcriptase)
    Protein kinase (Tyrosine-kinase (Janus kinase))
    3.1 Phosphodiesterase Acetylcholinesterase Ribonuclease
    3.2 Polygalacturonase Neuraminidase Alpha-glucosidase
    Hydrolase (EC 3)
    3.4 Protease: Exopeptidase (Dipeptidyl peptidase-4, ACE)
    Endopeptidase (Trypsin, Renin, Matrix metalloproteinase)
    3.5 Histone deacetylase Beta-lactamase

    Lyase (EC 4)

    4.1 Dopa decarboxylase


    4.2 Carbonic anhydrase

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