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Censavudine

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From Wikipedia, the free encyclopedia

Investigational new anti-HIV drug

Pharmaceutical compound

Censavudine
Clinical data


Other names	4'-ethynylstavudine, festinavir
Legal status
Legal status	Investigational
Identifiers
IUPAC name 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
CAS Number	634907-30-5
PubChemCID	3008897
ChemSpider	2278330
UNII	6IE83O6NGA
KEGG	D10550
ChEMBL	ChEMBL124363
NIAID ChemDB	209894
CompTox Dashboard(EPA)	DTXSID50212893
ECHA InfoCard	100.225.812
Chemical and physical data
Formula	C₁₂H₁₂N₂O₄
Molar mass	248.238 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=CN(C(=O)NC1=O)[C@H]2C=C[C@](O2)(CO)C#C
InChI InChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1 Key:OSYWBJSVKUFFSU-SKDRFNHKSA-N

Censavudine (INN;^[1] development codeBMS-986001) is aninvestigational new drug being developed byBristol Myers-Squibb for the treatment ofHIV infection.^[2]^[3] It was originally developed atYale University.^[4] It is still in an investigational phase of development as of 2023.^[5]

Renaming

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Until 2013, censavudine has been known asfestinavir, but the name was changed to avoid confusion with HIVprotease inhibitors which all bear class suffix "–navir" (e.g.tipranavir,lopinavir,saquinavir, etc.).^[5]

References

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^"International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 110"(PDF). World Health Organization. pp. 409–410.
^Wu VH, Smith RA, Masoum S, Raugi DN, Ba S, Seydi M, et al. (August 2017)."MK-8591 (4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture".Antimicrobial Agents and Chemotherapy.61 (8).doi:10.1128/AAC.00744-17.PMC 5527656.PMID 28559249.
^Gupta SK, McComsey GA, Lombaard J, Echevarría J, Orrell C, Avihingsanon A, et al. (January 2016). "Efficacy, safety, bone and metabolic effects of HIV nucleoside reverse transcriptase inhibitor BMS-986001 (AI467003): a phase 2b randomised, controlled, partly blinded trial".The Lancet. HIV.3 (1): e13-22.doi:10.1016/S2352-3018(15)00231-3.hdl:1805/10552.PMID 26762988.
^Alcorn K (21 December 2010)."Bristol-Myers Squibb buys festinavir, new NRTI active against MDR HIV".aidsmap.com.aidsmap. Retrieved24 June 2011.
^^a ^bPubChem."Censavudine".pubchem.ncbi.nlm.nih.gov. Retrieved2023-10-24.

Antiviral drugs:antiretroviral drugs used againstHIV (primarilyJ05)

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

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

°DHHSrecommendedinitial regimen options.^◊Formerly or rarely used agent.

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