Drug General Information
Drug ID D0A4IJ
Drug Name Abacavir
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 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: L74I [1]
Mutation Frequency 3-20% of the samples
Level of Resistance Reduce susceptibility to Abacavir
Mutation info Missense: K65R [2]
Level of Resistance Reduce ABC susceptibility 2 fold
Mutation info Missense: Y115F [3]
Level of Resistance Reduce ABC susceptibility 3 fold
Mutation info Missense: K65N [4], [5], [6]
Level of Resistance Reduce susceptibility to ABC
Mutation info Missense: L74V [7], [8], [9]
Level of Resistance Intermediate resistance
Mutation info Missense: K70E [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: K70G [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: K70N [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: K70Q [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: K70S [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: K70T [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: M184I [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: M184V [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: M41L [10], [11]
Mutation info Missense: Q151L [10], [11]
Level of Resistance Intermediate resistance
Mutation info Missense: Q151M [10], [11]
Level of Resistance Confer high-level resistance to ABC
Mutation info Missense: T210W [10], [11]
Mutation info Missense: T215F [10], [11]
Mutation info Missense: T215Y [10], [11]
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 Deletion: D67 [10], [11]
Level of Resistance Intermediate resistance
Mutation info Missense: D67E/G/N + K70R + M184I/V + K219E/N/Q/R [10], [11]
Level of Resistance Low-level resistance
Mutation info Deletion: K70 [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: L74I/V + M184I/V [10], [11]
Level of Resistance Low-level resistance
Mutation info Missense: M41L + T215F/Y [10], [11]
Level of Resistance Low-level resistance
Mutation info Deletion: S68 [10], [11]
Level of Resistance Low-level resistance
Mutation info Insertion: T69 [10], [11]
Level of Resistance Low-level resistance
Mutation info Deletion: T69 [10], [11]
Level of Resistance Low-level resistance
References
REF 1 Mechanisms of anti-retroviral drug resistance: implications for novel drug discovery and development. Infect Disord Drug Targets. 2013 Oct;13(5):330-6.
REF 2 In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA. Antivir Ther. 1999;4(2):87-94.
REF 3 Combination 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.
REF 4 A rare HIV reverse transcriptase mutation, K65N, confers reduced susceptibility to tenofovir, lamivudine and didanosine. AIDS. 2006 Mar 21;20(5):787-9.
REF 5 In 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.
REF 6 Reverse 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.
REF 7 Selection 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 8 Trends 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.
REF 9 HIV-1 Drug Resistance Mutations: Potential Applications for Point-of-Care Genotypic Resistance Testing. PLoS One. 2015 Dec 30;10(12):e0145772.
REF 10 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 11 Tackling the problem of HIV drug resistance. Postepy Biochem. 2016;62(3):273-279.

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