| Drug General Information |
| Drug ID |
D09SGV
|
| Drug Name |
Daclatasvir |
|
| Synonyms |
1009119-64-5; Daclatasvir (BMS-790052); 1214735-16-6; CHEBI:82977; C40H50N8O6; methyl N-[(1S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methyl-butanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidine-1-carbonyl]-2-methyl-propyl]carbamate; Daclatasvir (USAN); cc-39; Daclatasvir BMS 790052; MLS006011140; SCHEMBL2756027; CHEMBL2023898; SCHEMBL17897804; KS-00000XPC; EX-A410 |
| Drug Type |
Small molecular drug |
| Company |
Bristol-Myers Squibb |
| Structure |
|
| Drug Resistance Mutations |
| Target Name |
HCV Non-structural protein 5A (NS5A) |
Target Info |
| Gene Name |
NS5A |
| Uniprot ID |
POLG_HCV1(1973-2420) |
| Species |
Hepatitis C virus genotype 1a |
| Reference Sequence |
SGSWLRDIWDWICEVLSDFKTWLKAKLMPQLPGIPFVSCQRGYKGVWRVDGIMHTRCHCG
AEITGHVKNGTMRIVGPRTCRNMWSGTFPINAYTTGPCTPLPAPNYTFALWRVSAEEYVE
IRQVGDFHYVTGMTTDNLKCPCQVPSPEFFTELDGVRLHRFAPPCKPLLREEVSFRVGLH
EYPVGSQLPCEPEPDVAVLTSMLTDPSHITAEAAGRRLARGSPPSVASSSASQLSAPSLK
ATCTANHDSPDAELIEANLLWRQEMGGNITRVESENKVVILDSFDPLVAEEDEREISVPA
EILRKSRRFAQALPVWARPDYNPPLVETWKKPDYEPPVVHGCPLPPPKSPPVPPPRKKRT
VVLTESTLSTALAELATRSFGSSSTSGITGDNTTTSSEPAPSGCPPDSDAESYSSMPPLE
GEPGDPDLSDGSWSTVSSEANAEDVVCC [Hepatitis C virus genotype 1a]
|
| Targeted Disease |
HCV infection |
| Drug Resistance Mutations |
| Mutation info |
Missense: L31M |
[1], [2] |
| Level of Resistance |
Confer 3350 fold resistance |
|
| Mutation info |
Missense: L31V + Y93H |
[1], [2] |
| Level of Resistance |
Confer 8336 fold resistance |
|
| Mutation info |
Missense: L31V |
[1], [2] |
| Level of Resistance |
Confer 233 fold resistance |
|
| Mutation info |
Missense: M28T + Q30H |
[1], [2] |
| Level of Resistance |
Confer 8336 fold resistance |
|
| Mutation info |
Missense: M28T |
[1], [2] |
| Level of Resistance |
Confer 683 fold resistance |
|
| Mutation info |
Missense: P32L |
[1], [2] |
| Level of Resistance |
Confer 1850 fold resistance |
|
| Mutation info |
Missense: Q30E |
[1], [2] |
| Level of Resistance |
Confer 24933 fold resistance |
|
| Mutation info |
Missense: Q30H |
[1], [2] |
| Level of Resistance |
Confer 1450 fold resistance |
|
| Mutation info |
Missense: Q30R |
[1], [2] |
| Level of Resistance |
Confer 1217 fold resistance |
|
| Mutation info |
Missense: Y93C |
[1], [2] |
| Level of Resistance |
Confer 5367 fold resistance |
|
| Mutation info |
Missense: Y93H |
[1], [2] |
| Level of Resistance |
Confer 47477 fold resistance |
|
| Mutation info |
Missense: Y93N |
[1], [2] |
| Level of Resistance |
Confer 103767 fold resistance |
|
| References |
| REF 1 |
Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature. 2010 May 6;465(7294):96-100.
|
| REF 2 |
Resistance analysis of the hepatitis C virus NS5A inhibitor BMS-790052 in an in vitro replicon system. Antimicrob Agents Chemother. 2010 Sep;54(9):3641-50.
|
