BI 224436

BI 224436: BI 224436 is an investigational new drug under development for the treatment of HIV infection. BI 224436 is the first non-catalytic site integrase inhibitor (NCINI). It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct in mechanism of action compared to raltegravir and elvitegravir, which bind at the catalytic site.^[1] In October 2011, Gilead Sciences purchased exclusive rights to develop BI 224436 and several related compounds under investigation in Boehringer Ingelheim’s noncatalytic site integrase inhibitor program.^[2]^[3]

^ Levin, Jules. BI 224436, a Non-Catalytic Site Integrase Inhibitor, is a potent inhibitor of the replication of treatment-naïve and raltegravir-resistant clinical isolates of HIV-1. Conference Reports for NATAP. ICAAC Chicago Sept 17-20 2011.

^ Gilead Negotiates Worldwide License to BI’s Early Clinical Stage HIV Program. Genetic Engineering and Biotechnology News. 6 Oct 2011.

^ Highleyman, Liz. ICAAC: New Integrase Inhibitor BI 224436 Active against Raltegravir-Resistant HIV. HIVandHepatitis.com. 7 Oct 2011.

v · d · eAntiviral drugs: antiretroviral drugs used against HIV (primarily J05)

Entry/fusion inhibitors
(Discovery & development)
gp41 (Enfuvirtide) • CCR5 (Maraviroc, Vicriviroc^†, Cenicriviroc^†, PRO 140^†) • CD4 (Ibalizumab^†)

Reverse-transcriptase
inhibitors (RTIs)

Nucleoside &
Nucleotide (NRTI)

Nucleoside analogues/NARTIs: Abacavir (ABC)°^# • Emtricitabine (FTC)°^# • Lamivudine (3TC)°^# • Didanosine (ddI)^# • Zidovudine (AZT)^# • Apricitabine^† • Stampidine^† • Elvucitabine^† • Racivir^† • Amdoxovir^†• Stavudine (d4T)^# • Zalcitabine (ddC)^◊ • Festinavir^†
Nucleotide analogues/NtRTIs: Tenofovir°^# • GS 7340

Non-Nucleoside (NNRTI)
(Discovery & development)

(1^st generation) Efavirenz°^# • Nevirapine^# • Loviride^◊ • Delavirdine^◊ •
(2^nd generation) diarylpyrimidines (Etravirine, Rilpivirine) • Lersivirine^†

Integrase inhibitors
Raltegravir • Elvitegravir^† • Dolutegravir^† • Globoidnan A (experimental) • MK-2048^† • BI 224436^†

Maturation inhibitors
Bevirimat^† • Vivecon^†

Protease Inhibitors (PI)
(Discovery and development)

1^st generation

Fosamprenavir° • Lopinavir°^# • Nelfinavir^# • Ritonavir^# • Saquinavir^# • Amprenavir^◊ • Indinavir^◊^#

2^nd generation

Atazanavir° • Darunavir • Tipranavir

Combined formulations
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

Other

Abzyme • Calanolide A • Ceragenin • Cyanovirin-N • Diarylpyrimidines • Epigallocatechin gallate (EGCG) • Foscarnet • Griffithsin • Hydroxycarbamide • Miltefosine • Portmanteau inhibitors • Seliciclib^† • Synergistic enhancers • Tre recombinase • Zinc finger protein transcription factor • KP-1461^† • Cobicistat^†

Failed agents

Dexelvucitabine • Capravirine • Emivirine • Lodenosine • Atevirdine • Brecanavir • Aplaviroc

^#WHO-EM. ^‡Withdrawn from market. Clinical trials: ^†Phase III. ^§Never to phase III °DHHS preferred first-line agent. ^◊Formerly or rarely used agent.

M: VIR

virs(prot)/clss

cutn/syst (hppv/hiva, infl/zost/zoon)/epon

drugJ(dnaa, rnaa, rtva, vacc)

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