BIT225

BIT225
Names

IUPAC name N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
Other names BIT-225
Identifiers
CAS Number	917909-71-8^Y
3D model (JSmol)	Interactive image
ChemSpider	10176885
PubChem CID	12004418
UNII	M9C27TI12U^Y
InChI InChI=1S/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22) Key: WVROWPPEIMRGAB-UHFFFAOYSA-N InChI=1/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22) Key: WVROWPPEIMRGAB-UHFFFAOYAP
SMILES CN1C=C(C=N1)C2=CC=CC3=C2C=CC(=C3)C(=O)NC(=N)N
Properties
Chemical formula	C₁₆H₁₅N₅O
Molar mass	293.330 g·mol⁻¹
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

Chemical compound

BIT225 is an experimental drug candidate under development by Biotron Limited for use in the treatment of both HIV and hepatitis C infection. By blocking Vpu ion channel activity, it disrupts HIV assembly within host monocyte cells; its method of action is a first for HIV drugs.^[1] Because it targets replication in monocyte derived macrophages, it offers promise for treatment of viral reservoirs that are unaffected by standard treatments.^[2] The activity of BIT225 is post-virus integration, with no direct effects on the HIV enzymes reverse transcriptase and protease.^[3] Since Vpu ion channel activity is highly conserved, the virus is unlikely to become resistant via generation of Vpu ion-independent virus. In addition, the drug also has been credited with curing hepatitis C after 12 weeks of treatment.^[4]

References

^ BIT225 therapy reduces HIV-1 burden in monocyte cells and decreases immune activation
^ BIT225, a Novel Assembly Inhibitor, Cuts HIV Load in Monocyte Reservoir
^ Antiviral Efficacy of the Novel Compound BIT225 against HIV-1 Release from Human Macrophages
^ BIT225 Trial Results Show Effective Cure of Hepatitis C

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

Capsid inhibitors

Lenacapavir (LEN)

Entry/fusion inhibitors
(Discovery and development)

gp41 (Enfuvirtide (ENF, T-20))^◊
CCR5 (Maraviroc (MVC)
Vicriviroc^†, Cenicriviroc^†, Leronlimab^†)
CD4 (Ibalizumab (IBA), Semzuvolimab^§)
gp120 (Fostemsavir (FTR))

Integrase inhibitors
(Integrase strand transfer inhibitors (INSTI))

Maturation inhibitors

Protease Inhibitors (PI)
(Discovery and development)

1^st generation	Amprenavir (APV)^‡ Fosamprenavir (FPV) Indinavir (IDV)^◊ Lopinavir (LPV) Nelfinavir (NFV)^◊ Ritonavir (RTV)^# Saquinavir (SQV)^◊
2^nd generation	Atazanavir (ATV)°^# Darunavir (DRV)°^# Tipranavir (TPV)^◊ TMC-310911^§

Reverse-transcriptase
inhibitors (RTIs)

Nucleoside and
nucleotide (NRTI)

Nucleoside analogues/NRTIs: Abacavir (ABC)^#
Didanosine (ddI)^◊
Emtricitabine (FTC)
Lamivudine (3TC)^#
Stavudine (d4T)^◊
Zalcitabine (ddC)^‡
Zidovudine (AZT, ZDV)^#
Amdoxovir^†
Apricitabine^†
Censavudine^†
Elvucitabine^†
Islatravir (EFdA, ISL)^§
Racivir^†
Stampidine^†

Non-nucleoside (NNRTI)
(Discovery and development)

1^st generation	Efavirenz (EFV)^# Nevirapine (NVP)^# Delavirdine (DLV)^‡
2^nd generation	diarylpyrimidines Dapivirine (DPV) Etravirine (ETR) Rilpivirine (RPV) Doravirine (DOR) Elsulfavirine (ESV)

Combined formulations

Pharmacokinetic boosters

Experimental agents

Uncoating inhibitors	TRIM5alpha (gene)
Transcription inhibitors	Tat antagonists
Translation inhibitors	Trichosanthin
BNAbs	Elipovimab
Other	Abzyme BIT225^† Calanolide A Ceragenin Cyanovirin-N Diarylpyrimidines Epigallocatechin gallate (EGCG) Foscarnet Fosdevirine^† Griffithsin Hydroxycarbamide KP-1461^† Miltefosine Portmanteau inhibitors Scytovirin Seliciclib^† Synergistic enhancers Tre recombinase Zinc finger protein transcription factor
Failed agents	Aplaviroc Atevirdine Brecanavir Capravirine Dexelvucitabine Droxinavir Lasinavir Emivirine Lersivirine Lodenosine Loviride Mozenavir Palinavir Telinavir