Censavudine

Category	Reverse Transcriptases (RTs)
CAS	634907-30-5
Description	Censavudine is a nucleoside reverse transcriptase inhibitor. It is active against HIV resistant to both abacavir and tenofovir. It is a candidate for people with multi-drug resistant (MDR) strains of the virus. It is a derivative of stavudine (d4T), but is less toxic. It has demonstrated potent in vitro activity against HIV-2. It was developed by Bristol Myers-Squibb and in clinic phase 2 trials.

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Product Information

Synonyms	OBP-601; OBP601; OBP 601; BMS-986001; BMS 986001; BMS986001; festinavir; 4'-Ed4T; Censavudine; 2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine;4'-Ed4T;4'-Ethynylstavudine;4'-Ethynyl D4T;1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione;
IUPAC Name	1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
Molecular Weight	248.24
Molecular Formula	C12H12N2O4
Canonical SMILES	CC1=CN(C(=O)NC1=O)C2C=CC(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
InChIKey	OSYWBJSVKUFFSU-SKDRFNHKSA-N
Melting Point	207-209 °C
Purity	98%
Density	1.42±0.1 g/cm3 \| Condition: Temp: 20 °C Press: 760 Torr
Solubility	Soluble in DMSO, not in water
Appearance	Solid powder
Application	Censavudine is active against HIV resistant to both abacavir and tenofovir.
Storage	-20°C Freezer
Complexity	513
Exact Mass	248.07970687
In Vitro	BMS-986001 shows greater activity against HIV-2ROD9 than against HIV-1NL4-3; the mean EC50s for BMS-986001 are 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3 in the single-cycle assay. HIV-2ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC50 for HIV-2ROD9 (EC50 of 0.14 nM) being 30-fold lower than that for HIV-1NL4-3 (EC50 of 4.2 nM). BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase.
In Vivo	The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC(0-24 h) and C max for BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h.
PSA	84.58000
Target	HIV-2:30-81 nM (EC50) HIV-1:450-890 nM (IC50)
XLogP3-AA	-0.7