Resistance mutation info of drug

Drug General Information
Drug ID D0A4IJ
Drug Name Abacavir Drug Info
Synonyms Trizivir; Ziagen; Abacavir [INN]; Abacavir (INN); Ziagen (TN); Ziagen (TM)(*Succinate salt*); [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol; {(1S-cis)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopent-2-en-1-yl}methanol; (+/-)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol; (+/-)-Abacavir; (1S,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol; ABC
Drug Type Small molecular drug
Therapeutic Class Anti-HIV Agents
Company GlaxoSmithKline
Structure D0A4IJ
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 Deletion: D67 [556228], [556244]
Level of Resistance Intermediate resistance
Mutation info Missense: D67E/G/N + K70R + M184I/V + K219E/N/Q/R [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Deletion: K70 [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: L74I/V + M184I/V [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: M41L + T215F/Y [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Deletion: S68 [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Insertion: T69 [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Deletion: T69 [556228], [556244]
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
Level of Resistance Reduce susceptibility to Abacavir
Mutation info Missense: K65R [555464]
Level of Resistance Reduce ABC susceptibility 2 fold
Mutation info Missense: Y115F [556204]
Level of Resistance Reduce ABC susceptibility 3 fold
Mutation info Missense: K65N [555588], [555609], [555801]
Level of Resistance Reduce susceptibility to ABC
Mutation info Missense: L74V [555647], [555958], [556100]
Level of Resistance Intermediate resistance
Mutation info Missense: K70E [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: K70G [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: K70N [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: K70Q [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: K70S [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: K70T [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: M184I [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: M184V [556228], [556244]
Level of Resistance Low-level resistance
Mutation info Missense: M41L [556228], [556244]
Mutation info Missense: Q151L [556228], [556244]
Level of Resistance Intermediate resistance
Mutation info Missense: Q151M [556228], [556244]
Level of Resistance Confer high-level resistance to ABC
Mutation info Missense: T210W [556228], [556244]
Mutation info Missense: T215F [556228], [556244]
Mutation info Missense: T215Y [556228], [556244]
References
Ref 550653Abacavir (marketed as Ziagen) and Abacavir-containing Medications. FDA. 2008.
Ref 555464In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA. Antivir Ther. 1999;4(2):87-94.
Ref 555588A rare HIV reverse transcriptase mutation, K65N, confers reduced susceptibility to tenofovir, lamivudine and didanosine. AIDS. 2006 Mar 21;20(5):787-9.
Ref 555609In vitro human immunodeficiency virus type 1 resistance selections with combinations of tenofovir and emtricitabine or abacavir and lamivudine. Antimicrob Agents Chemother. 2006 Dec;50(12):4087-95. Epub 2006 Sep 18.
Ref 555647Selection of L74V mutation in reverse transcriptase of HIV-1 subtype D by a tenofovir DF-lamivudine based regimen. AIDS. 2007 Nov 30;21(18):2551-2.
Ref 555801Reverse transcriptase mutation K65N confers a decreased replication capacity to HIV-1 in comparison to K65R due to a decreased RT processivity. Virology. 2011 May 25;414(1):34-41. doi: 10.1016/j.virol.2011.03.007. Epub 2011 Apr 2.
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 555958Trends in Genotypic HIV-1 Antiretroviral Resistance between 2006 and 2012 in South African Patients Receiving First- and Second-Line Antiretroviral Treatment Regimens. PLoS One. 2013 Jun 26;8(6):e67188. doi: 10.1371/journal.pone.0067188. Print 2013.
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 556100HIV-1 Drug Resistance Mutations: Potential Applications for Point-of-Care Genotypic Resistance Testing. PLoS One. 2015 Dec 30;10(12):e0145772. doi: 10.1371/journal.pone.0145772. eCollection 2015.
Ref 556244Tackling the problem of HIV drug resistance. Postepy Biochem. 2016;62(3):273-279.
Ref 556204Combination of mutations in human immunodeficiency virus type 1 reverse transcriptase required for resistance to the carbocyclic nucleoside 1592U89. Antimicrob Agents Chemother. 1997 May;41(5):1094-8.

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