| Drug General Information |
| Drug ID |
D0X9CH
|
| Drug Name |
Telaprevir |
|
| Synonyms |
402957-28-2; VX-950; Incivek; Telaprevir (VX-950); Incivo; MP-424; VX 950; Telavic; VX-950(Telaprevir); LY-570310; UNII-655M5O3W0U; VRT-111950; CHEMBL231813; CHEBI:68595; 655M5O3W0U; S-Telaprevir; (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-6-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-octahydrocyclopenta[c]pyrrole-1-carboxamide |
| Drug Type |
Small molecular drug |
| 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: A156F |
[1], [2], [3] |
| Level of Resistance |
Confer >62 fold resistance |
|
| Mutation info |
Missense: A156N |
[1], [2], [3] |
| Level of Resistance |
Confer >93 fold resistance |
|
| Mutation info |
Missense: A156S |
[1], [2], [3] |
| Level of Resistance |
Confer 9.6 fold resistance |
|
| Mutation info |
Missense: A156T |
[1], [2], [3] |
| Level of Resistance |
Confer >62 fold resistance |
|
| Mutation info |
Missense: A156V |
[1], [2], [3] |
| Level of Resistance |
Confer >62 fold resistance |
|
| Mutation info |
Missense: D168N |
[1], [2], [3] |
| Level of Resistance |
Confer 0.63 fold resistance |
|
| Mutation info |
Missense: I132V |
[1], [2], [3] |
| Level of Resistance |
Confer 1.8 fold resistance |
|
| Mutation info |
Missense: R155G |
[1], [2], [3] |
| Level of Resistance |
Confer 7.4 fold resistance |
|
| Mutation info |
Missense: R155K |
[1], [2], [3] |
| Level of Resistance |
Confer 7.4 fold resistance |
|
| Mutation info |
Missense: R155M |
[1], [2], [3] |
| Level of Resistance |
Confer 5.6 fold resistance |
|
| Mutation info |
Missense: R155T |
[1], [2], [3] |
| Level of Resistance |
Confer 20 fold resistance |
|
| Mutation info |
Missense: T54A |
[1], [2], [3] |
| Level of Resistance |
Confer 6.3 fold resistance |
|
| Mutation info |
Missense: T54S |
[1], [2], [3] |
| Level of Resistance |
Confer 4.2 fold resistance |
|
| Mutation info |
Missense: V36A |
[1], [2], [3] |
| Level of Resistance |
Confer 7.4 fold resistance |
|
| Mutation info |
Missense: V36G |
[1], [2], [3] |
| Level of Resistance |
Confer 11 fold resistance |
|
| Mutation info |
Missense: V36I |
[1], [2], [3] |
| Level of Resistance |
Confer 0.3 fold resistance |
|
| Mutation info |
Missense: V36L |
[1], [2], [3] |
| Level of Resistance |
Confer 2.2 fold resistance |
|
| Mutation info |
Missense: V36M + R155K |
[1], [2], [3] |
| Level of Resistance |
Confer ~64 fold resistance |
|
| Mutation info |
Missense: V36M |
[1], [2], [3] |
| Level of Resistance |
Confer 7 fold resistance |
|
| References |
| REF 1 |
In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistan... J Biol Chem. 2004 Apr 23;279(17):17508-14.
|
| REF 2 |
In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061. J Biol Chem. 2005 Nov 4;280(44):36784-91.
|
| REF 3 |
Hepatitis C viral evolution in genotype 1 treatment-nae and treatment-experienced patients receiving telaprevir-based therapy in clinical trials. PLoS One. 2012;7(4):e34372.
|
