Resistance mutation info of drug

Drug General Information
Drug ID D0S9SD
Drug Name Emtricitabine Drug Info
Synonyms Coviracil; DOTFC; Emtriva; RCV; Racivir; BW 1592; BW 524W91; BW524W91; Atripla (TN); BW-524W91; Coviracil (TN); Coviracil(TM); DRG-0208; Emtriva (TN); Emtriva(TM); Truvada (TN); 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
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 [556228], [556236]
Mutation info Deletion: D67 [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Deletion: K70 [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Deletion: S68 [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Insertion: T69 [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Deletion: T69 [556228], [556237]
Level of Resistance Low-level resistance
Target Name HIV Nucleoside reverse transcriptase
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: L74I [556230]
Mutation Prevalence 3-20% of the samples
Mutation info Missense: F77L + F116Y + Q151M [556228], [556236]
Level of Resistance Low-level resistance
Mutation info Missense: K65N [556228], [556236]
Level of Resistance Low-level resistance
Mutation info Missense: M184I [556228], [556236]
Level of Resistance High-level resistance
Mutation info Missense: M184V [556228], [556236]
Level of Resistance High-level resistance
Mutation info Missense: Q151M [556228], [556236]
Level of Resistance Confer low-level resistance to FTC
References
Ref 527650Emtricitabine: a novel nucleoside reverse transcriptase inhibitor. Drugs Today (Barc). 2005 Apr;41(4):241-52.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 556228The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101. doi: 10.1159/000331998. Epub 2012 Jan 24.
Ref 556230Mechanisms of anti-retroviral drug resistance: implications for novel drug discovery and development. Infect Disord Drug Targets. 2013 Oct;13(5):330-6.
Ref 556236Global burden of transmitted HIV drug resistance and HIV-exposure categories: a systematic review and meta-analysis. AIDS. 2014 Nov 28;28(18):2751-62. doi: 10.1097/QAD.0000000000000494.
Ref 556237Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71. doi: 10.1038/nrg3922. Epub 2015 Jul 7.

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