Resistance mutation info of drug

Drug General Information
Drug ID D0S9SD
Drug Name Emtricitabine
Synonyms Coviracil; DOTFC; Emtriva; RCV; Racivir; BW 1592; BW 524W91; BW524W91; BW-524W91; Coviracil (TN); Coviracil(TM); DRG-0208; Emtriva(TM); Emtricitabine (JAN/USAN/INN); Beta-L-2',3'-dideoxy-5-fluoro-3'-thiacytidine; Beta-L-(-)-(2R,5S)-5-Fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine; (-)-(2R,5S)-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine; (-)-.beta.-L-FTC; (-)-2',3'-Dideoxy-5-fluoro-3'-thiacytidine; (-)-2'-Deoxy-5-fluoro-3'-thiacytidine; (-)-FTC; (-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine; (-)-cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one; (2R-cis)-4-Amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2(1H)-pyrimidinone; 1-(2-(Hydroxymethyl)oxathiolan-5-yl)-5-fluorocytosine; 2',3',5-FTC; 2',3'-Dideoxy-5-fluoro-3'-thiacytidine; 2'-Deoxy-5-fluoro-3'-oxa-4'-thiocytidine; 2'-Deoxy-5-fluoro-3'-thiacytidine; 2-FTC; 3'-Thia-2'.3'-dideoxy-5-fluorocytidine; 4-Amino-5-fluoro-1-[(2R,5S)-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone; 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2(1H)-one; 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one; 5-Fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)cytosine; 5-Fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)cytosine; 5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)[1,3]oxathiolan-5-yl]cytosine; 524W91; FTC
Drug Type Small molecular drug
Therapeutic Class Anti-HIV Agents
Company Gilead; Bristol-Myers Squibb
Structure D0S9SD
Drug Resistance Mutations
Target Name HIV Non-Nucleoside reverse transcriptase Target Info
Uniprot ID POL_HV1B1(600-1159)
Species Human immunodeficiency virus type 1 (HIV-1)
Reference Sequence PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKIL [Human immunodeficiency virus type 1 (H
IV-1)]
Targeted Disease HIV infection
Drug Resistance Mutations
Mutation info Missense: K65R [1], [2]
Mutation info Deletion: D67 [1], [3]
Level of Resistance Low-level resistance
Mutation info Deletion: K70 [1], [3]
Level of Resistance Low-level resistance
Mutation info Deletion: S68 [1], [3]
Level of Resistance Low-level resistance
Mutation info Insertion: T69 [1], [3]
Level of Resistance Low-level resistance
Mutation info Deletion: T69 [1], [3]
Level of Resistance Low-level resistance
Target Name HIV Nucleoside reverse transcriptase Target Info
Uniprot ID POL_HV1B1(600-1159)
Species Human immunodeficiency virus type 1 (HIV-1)
Reference Sequence PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTN [Human immunodefici
ency virus type 1 (HIV-1)]
Targeted Disease HIV infection
Drug Resistance Mutations
Mutation info Missense: F77L + F116Y + Q151M [1], [2]
Level of Resistance Low-level resistance
Mutation info Missense: K65N [1], [2]
Level of Resistance Low-level resistance
Mutation info Missense: M184I [1], [2]
Level of Resistance High-level resistance
Mutation info Missense: M184V [1], [2]
Level of Resistance High-level resistance
Mutation info Missense: Q151M [1], [2]
Level of Resistance Confer low-level resistance to FTC
Mutation info Missense: L74I [4]
Mutation Frequency 3-20% of the samples
References
REF 1 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 2 Global burden of transmitted HIV drug resistance and HIV-exposure categories: a systematic review and meta-analysis. AIDS. 2014 Nov 28;28(18):2751-62.
REF 3 Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71.
REF 4 Mechanisms of anti-retroviral drug resistance: implications for novel drug discovery and development. Infect Disord Drug Targets. 2013 Oct;13(5):330-6.

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