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.^[2] 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.^[3]^[4]

References

Entry/fusion inhibitors
(Discovery & development)

gp41 (Enfuvirtide) • CCR5 (Maraviroc, Vicriviroc^†, Cenicriviroc^†, PRO 140^†) • CD4 (Ibalizumab^†)

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^†

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

Protease Inhibitors (PI)
(Discovery and development)

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

2^nd generation	Atazanavir° • Darunavir • Tipranavir

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 ^‡Withdrawn from market.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.

virs(prot)/clss

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

drugJ(dnaa, rnaa, rtva, vacc)