Resistance mutation info of drug

Drug General Information

Drug ID

D07TQV

Drug Name

Lamivudine

Synonyms

lamivudine; 134678-17-4; Epivir; Zeffix; Heptovir; Epivir-HBV; Hepitec; Heptodin; BCH-189; 3TC; Heptivir; CIS-LAMIVUDINE; (-)-2'-Deoxy-3'-thiacytidine; 4-amino-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one; GR-109714X; 3'-Thia-2',3'-dideoxycytidine; (-)-BCH-189; Lamivudine [USAN:BAN:INN]; GR109714X; beta-L-3'-Thia-2',3'-dideoxycytidine; beta-L-2',3'-Dideoxy-3'-thiacytidine; (-)NGPB-21; 136891-12-8; 2',3'-Dideoxy-3'-thiacytidine; (-)-BCH 189; UNII-2T8Q726O95; HSDB 7155; GR 109714X; DTHC; LMV; Lamivir; Zefix; BCH 189; BCH189; BCH-790; DRG-0126; Epivir (TN); Epivir(TM); GG-714; HHA & 3TC; HHA & Lamivudine; Heptovir (TN); Lamivudine & GNA; Zeffix (TN); Epivir-HBV (TN); Lamivudine [USAN:INN:BAN]; Lamivudine (JAN/USP/INN); Lamivudine, (2S-cis)-Isomer; Beta-L-2',3'-Dideoxy-3'-thiacytidine; Beta-L-3'-Thia-2',3'-dideoxycytidine; Beta-L-(-)-2',3'-dideoxy-3'-thiacytidine & Sho-Saiko-To; (+/-)-(Cis)-1-[2-(Hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine; (+/-)-3TC; (+/-)-BCH-189; (+/-)-SddC; (-)-(2'R,5'S)-1-[2'-Hydroxymethyl-5'-(1,3-oxathiolanyl)]cytosine; (-)-1-((2R,5S)-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl)cytosine; (-)-1-[(2R,5S)-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine; (-)-NGPB-21; (-)-SddC; (-)-beta-L-2',3'-Dideoxy-3'-thiacytidine; (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one; 2',3' Dideoxy 3' thiacytidine; 2(1H)-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl], (+/-)-(Cis); 2(1H)-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl], (-)-(2R,5S); 2(1H)-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl], (-)-(2R,5S) & Galanthus Nivalis Agglutinin (GNA); 2(1H)-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl], (-)-(2R,5S) & Hippeastrum hybrid agglutinin(HHA); 3TC & GNA; 3TC & SST; 3TC (AIDS INITIATIVE) (AIDS INITIATIVE); 3TC and NV-01; 3TC, Zeffix, Heptovir, Epivir, Epivir-HBV, Lamivudine; 4-Amino-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2(1H)-pyrimidinone; 4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2(1H)-one; 4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one; Efavirenz/lamivudine/tenofovir fumarate

Drug Type

Small molecular drug

Therapeutic Class

Anti-HIV Agents

Company

Glaxo Smith Kline Pharmaceuticals

Structure

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; HBV infection

Drug Resistance Mutations

Mutation info	Missense: K65N				[1], [2]
Level of Resistance	Low-level resistance

Mutation info	Missense: K65R				[1], [2]
Level of Resistance	Intermediate 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 3TC

Mutation info	Missense: F77L + F116Y + Q151M				[1], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: L74I				[4]
Mutation Frequency	3-20% of the samples

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

Targeted Disease

HIV infection; HBV infection

Drug Resistance Mutations

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

HBV Reverse transcriptase

Target Info

Uniprot ID

DPOL_HBVB5(347-690)

Species

Hepatitis B virus genotype B (HBV-B)

Reference Sequence

EDWGPCTEHGEHRIRTPRTPARVTGGVFLVDKNPHNTTESRLVVDFSQFSRGNTRVSWPK
FAVPNLQSLTNLLSSNLSWLSLDVSAAFYHLPLHPAAMPHLLVGSSGLSRYVARLSSNSR
IINNQHRTMQNLHNSCSRNLYVSLMLLYKTYGRKLHLYSHPIILGFRKIPMGVGLSPFLL
AQFTSAICSVVRRAFPHCLAFSYMDDVVLGAKSVQHLESLYAAVTNFLLSLGIHLNPHKT
KRWGYSLNFMGYVIGSWGTLPQEHIVQKIKMCFRKLPVNRPIDWKVCQRIVGLLGFAAPF
TQCGYPALMPLYACIQAKQAFTFSPTYKAFLSKQYLNLYPVARQ [Hepatitis B vi
rus genotype B (HBV-B)]

Targeted Disease

HIV infection; HBV infection

Drug Resistance Mutations

Mutation info	Missense: M204V				[5]

References

REF 1

The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.

REF 2

How to win the HIV-1 drug resistance hurdle race: running faster or jumping higher Biochem J. 2017 Apr 26;474(10):1559-1577.

REF 3

Clinical correlates and molecular basis of HIV drug resistance. J Acquir Immune Defic Syndr. 1993;6 Suppl 1:S36-46.

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.

REF 5

Comparison of Detection Rate and Mutational Pattern of Drug-Resistant Mutations Between a Large Cohort of Genotype B and Genotype C Hepatitis B Virus-Infected Patients in North China. Microb Drug Resist. 2017 Jun;23(4):516-522.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Feng ZHU

Prof. Yuzong CHEN