| Drug General Information |
|---|
| Drug ID |
D06KJQ |
| Drug Name |
Bi-201335 |
Drug Info
|
| Drug Type |
Small molecular drug |
| Company |
Boehringer Ingelheim Pharma |
| Structure |
|
| Drug Resistance Mutations |
|---|
| Target Name |
HCV Serine protease (NS3) |
|
| 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 |
[555772],
[555824]
|
| Level of Resistance |
Confer 270 fold resistance |
|
| Mutation info |
Missense: A156V |
[555772],
[555824]
|
| Level of Resistance |
Confer 150 fold resistance |
|
| Mutation info |
Missense: D168A |
[555772],
[555824]
|
| Level of Resistance |
Confer 690 fold resistance |
|
| Mutation info |
Missense: D168G |
[555772],
[555824]
|
| Level of Resistance |
Confer 80 fold resistance |
|
| Mutation info |
Missense: D168V |
[555772],
[555824]
|
| Level of Resistance |
Confer 620 fold resistance |
|
| Mutation info |
Missense: Q80K |
[555772],
[555824]
|
| Level of Resistance |
Confer 2.2 fold resistance |
|
| Mutation info |
Missense: Q80L |
[555772],
[555824]
|
| Level of Resistance |
Confer 1.2 fold resistance |
|
| Mutation info |
Missense: Q80N |
[555772],
[555824]
|
| Level of Resistance |
Confer 0.6 fold resistance |
|
| Mutation info |
Missense: Q80R |
[555772],
[555824]
|
| Level of Resistance |
Confer 2.6 fold resistance |
|
| Mutation info |
Missense: R155K |
[555772],
[555824]
|
| Level of Resistance |
Confer 350 fold resistance |
|
| Mutation info |
Missense: R155Q |
[555772],
[555824]
|
| Level of Resistance |
Confer 60 fold resistance |
|
| Mutation info |
Missense: T54A |
[555772],
[555824]
|
| Level of Resistance |
Confer 0.9 fold resistance |
|
| Mutation info |
Missense: T54S |
[555772],
[555824]
|
| Level of Resistance |
Confer 3.5 fold resistance |
|
| Mutation info |
Missense: V36M |
[555772],
[555824]
|
| Level of Resistance |
Confer 2.1 fold resistance |
|
| References |
|---|
| Ref 550385 | 2011 Pipeline of Boehringer Ingelheim Pharma. |
|---|
| Ref 555772 | 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. doi: 10.1128/AAC.00787-10. Epub 2010 Sep 7. |
|---|
| Ref 555824 | In vitro resistance profile of the hepatitis C virus NS3 protease inhibitor BI 201335. Antimicrob Agents Chemother. 2012 Jan;56(1):569-72. doi: 10.1128/AAC.05166-11. Epub 2011 Oct 24. |
|---|
