| Drug General Information |
| Drug ID |
D06KJQ
|
| Drug Name |
BI 201335 |
|
| Synonyms |
Faldaprevir; BI-201335; UNII-958X4J301A; CHEMBL1241348; 958X4J301A; N-[(Cyclopentyloxy)carbonyl]-3-Methyl-L-Valyl-(4r)-4-[(8-Bromo-7-Methoxy-2-{2-[(2-Methylpropanoyl)amino]-1,3-Thiazol-4-Yl}quinolin-4-Yl)oxy]-N-[(1r,2s)-1-Carboxy-2-Ethenylcyclopropyl]-L-Prolinamide; BI 201335; 801283-95-4; BI201335; Faldaprevir [USAN:INN]; SCHEMBL222429; BDBM50336545; SB16712; DB11808 |
| Drug Type |
Small molecular drug |
| Company |
Boehringer Ingelheim Pharma |
| Structure |
|
| Drug Resistance Mutations |
| Target Name |
HCV Serine protease (NS3) |
Target Info |
| Gene Name |
NS3 |
| Uniprot ID |
POLG_HCVJA(1027-1657) |
| Species |
Hepatitis C virus genotype 1b |
| Reference Sequence |
APITAYSQQTRGLLGCIITSLTGRDKNQVDGEVQVLSTATQSFLATCVNGVCWTVYHGAG
SKTLAGPKGPITQMYTNVDQDLVGWPAPPGARSMTPCTCGSSDLYLVTRHADVVPVRRRG
DSRGSLLSPRPISYLKGSSGGPLLCPSGHVVGIFRAAVCTRGVAKAVDFIPVESMETTMR
SPVFTDNSSPPAVPQTFQVAHLHAPTGSGKSTKVPAAYAAQGYKVLVLNPSVAATLGFGA
YMSKAHGIEPNIRTGVRTITTGGPITYSTYCKFLADGGCSGGAYDIIICDECHSTDSTTI
LGIGTVLDQAETAGARLVVLATATPPGSITVPHPNIEEVALSNTGEIPFYGKAIPIEAIK
GGRHLIFCHSKKKCDELAAKLTGLGLNAVAYYRGLDVSVIPTSGDVVVVATDALMTGFTG
DFDSVIDCNTCVTQTVDFSLDPTFTIETTTLPQDAVSRAQRRGRTGRGRSGIYRFVTPGE
RPSGMFDSSVLCECYDAGCAWYELTPAETSVRLRAYLNTPGLPVCQDHLEFWESVFTGLT
HIDAHFLSQTKQAGDNLPYLVAYQATVCARAQAPPPSWDQMWKCLIRLKPTLHGPTPLLY
RLGAVQNEVTLTHPITKYIMACMSADLEVVT [Hepatitis C virus genotype
1b]
|
| Targeted Disease |
HCV infection |
| Drug Resistance Mutations |
| Mutation info |
Missense: A156T |
[1], [2] |
| Level of Resistance |
Confer 270 fold resistance |
|
| Mutation info |
Missense: A156V |
[1], [2] |
| Level of Resistance |
Confer 150 fold resistance |
|
| Mutation info |
Missense: D168A |
[1], [2] |
| Level of Resistance |
Confer 690 fold resistance |
|
| Mutation info |
Missense: D168G |
[1], [2] |
| Level of Resistance |
Confer 80 fold resistance |
|
| Mutation info |
Missense: D168V |
[1], [2] |
| Level of Resistance |
Confer 620 fold resistance |
|
| Mutation info |
Missense: Q80K |
[1], [2] |
| Level of Resistance |
Confer 2.2 fold resistance |
|
| Mutation info |
Missense: Q80L |
[1], [2] |
| Level of Resistance |
Confer 1.2 fold resistance |
|
| Mutation info |
Missense: Q80N |
[1], [2] |
| Level of Resistance |
Confer 0.6 fold resistance |
|
| Mutation info |
Missense: Q80R |
[1], [2] |
| Level of Resistance |
Confer 2.6 fold resistance |
|
| Mutation info |
Missense: R155K |
[1], [2] |
| Level of Resistance |
Confer 350 fold resistance |
|
| Mutation info |
Missense: R155Q |
[1], [2] |
| Level of Resistance |
Confer 60 fold resistance |
|
| Mutation info |
Missense: T54A |
[1], [2] |
| Level of Resistance |
Confer 0.9 fold resistance |
|
| Mutation info |
Missense: T54S |
[1], [2] |
| Level of Resistance |
Confer 3.5 fold resistance |
|
| Mutation info |
Missense: V36M |
[1], [2] |
| Level of Resistance |
Confer 2.1 fold resistance |
|
| References |
| REF 1 |
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease. Antimicrob Agents Chemother. 2010 Nov;54(11):4611-8.
|
| REF 2 |
In vitro resistance profile of the hepatitis C virus NS3 protease inhibitor BI 201335. Antimicrob Agents Chemother. 2012 Jan;56(1):569-72.
|
