HIV Detail Information

Cabotegravir (ID: DG00116) Resistance Data of HIV
Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Resistant Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.E11D+p.S17C+p.L68V+p.L101I+p.T124N+p.T125A+p.I135V+p.G140A+p.Q148R+p.D253E+p.V281M
Missense mutation 21.7 Low-level resistance [1]
Resistant Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q181H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Resistant Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.E11D+p.K14R+p.S17T+p.V31I+p.L45V+p.A91S+p.L101I+p.T124A+p.E138Q+p.G140C+p.Q148R+p.V151I+p.K219N+p.N222K+p.L234I+p.V259I
Missense mutation 66.3 High-level resistance [1]
Resistant Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q182H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Resistant Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.S24G+p.D25E+p.S39C+p.I60IM+p.L63I+p.T97A+p.L101I+p.S119SR+p.T124N+p.T125A+p.I135V+p.E138T+p.G140S+p.Q148H+p.M154I+p.V165I+p.V201I+p.V259VI
Missense mutation 100 High-level resistance [1]
Resistant Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q183H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Resistant Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.D6T+p.K7E+p.S17N+p.V54I+p.I72V+p.L74M+p.V79I+p.T97A+p.L101I+p.I113L+p.S119R+p.T122I+p.T124N+p.T125A+p.E138K+p.G140A+p.I141AT+p.S147SG+p.Q148R+p.K156N+p.I203M+p.I208M+p.L234V+p.D253E
Missense mutation 100 High-level resistance [1]
Resistant Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q184H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Resistant Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.E69ED+p.E138K+p.G140S+p.Q148H+p.M154I+p.N155H+p.V201I
Missense mutation 100 High-level resistance [1]
Resistant Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q185H/k/R plus one to two additional INSTI mutations.
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.S24H+p.V31I+p.L68I+p.I73V+p.E92Q+p.L101I+p.T112V+p.S119T+p.T124G+p.T125A+p.G134N+p.K136T+p.V165I+p.V201I+p.T206S+p.L234I+p.D256E+p.S283G
Missense mutation 0.8 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q167H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.S17N+p.S39R+p.L45V+p.M50ML+p.T66A+p.V75I+p.L101I+p.T124A+p.K127R+p.S147SG+p.G163K+p.V201I
Missense mutation 0.8 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q168H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.A23T+p.S24G+p.D25E+p.L28I+p.I72V+p.T124A+p.Q148R+p.V165I+p.L172LF+p.H183HP+p.Q209QP+p.A239AT
Missense mutation 1.2 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q169H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K7KR+p.S17N+p.I72V+p.I84L+p.T97A+p.L101I+p.T112I+p.S119P+p.T122I+p.T124N+p.T125A+p.K136Q+p.Y143R+p.V201I+p.A205S+p.K211R+p.T218L+p.L234V+p.D256E+p.I268L+p.D270H
Missense mutation 1.2 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q170H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.S17N+p.M154L+p.N155H+p.V201I+p.D232N+p.L242LF
Missense mutation 1.3 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q171H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.E11D+p.R20K+p.E92Q+p.V201I+p.K211R+p.S230SN+p.D232E+p.D256E
Missense mutation 1.3 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q172H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.L101V+p.T112I+p.T125V+p.N155H+p.E157Q+p.K160Q+p.G193E+p.S230N+p.L234I+p.A265V+p.D279G
Missense mutation 1.6 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q173H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.V31I+p.V32I+p.L45Q+p.L101I+p.T112V+p.T125A+p.G134N+p.I135V+p.K136T+p.Y143C+p.V201I+p.T206S+p.S230R+p.L234I+p.N254NS+p.R269K+p.D270H
Missense mutation 2.2 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q174H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.E11D+p.V31I+p.G70R+p.I84V+p.L101I+p.S119P+p.T122I+p.N155H+p.G163E+p.V201I+p.D256E
Missense mutation 2.3 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q175H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.E10D+p.S17T+p.S39N+p.I72V+p.S119P+p.T122I+p.T124N+p.T125A+p.V151I+p.N155H+p.N222K+p.P261A
Missense mutation 2.3 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q176H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.S17N+p.D25E+p.S119G+p.T122I+p.T124N+p.T125A+p.M154I+p.N155H+p.K156R+p.T206S+p.T218S
Missense mutation 2.5 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q177H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.K14R+p.V31I+p.T97A+p.L101I+p.T112V+p.S119R+p.T124A+p.T125S+p.G134N+p.K136T+p.N155H+p.V165I+p.V201I+p.T206S+p.Y227F+p.L234I+p.S255N+p.D256E+p.S283G
Missense mutation 3 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q178H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.S17N+p.R20K+p.M50I+p.V77A+p.L101I+p.T112I+p.T124A+p.T125A+p.K136Q+p.G193E+p.V201I+p.T206S+p.T218L+p.I220V+p.L234V+p.D256E+p.R263K+p.D279G+p.S283G
Missense mutation 3.5 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q179H/k/R plus one to two additional INSTI mutations.
Key Molecule: HIV1 Integrase (HIV1 IT)
 Molecule Info 
Sensitive Disease Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration
Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref
p.G59D+p.I60V+p.E138K+p.Q148R+p.K173R+p.T218S+p.S230N+p.M275S+p.C280S
Missense mutation 9.9 Susceptible [1]
Sensitive Drug Cabotegravir
 Drug Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model TZM-bl cells Uterus Homo sapiens (Human) CVCL_B478
Experiment for
Molecule Alteration		 Population sequencing of the integrase region assay
Experiment for
Drug Resistance		 TZM-bl cell line-based phenotypic assay
Mechanism Description In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q180H/k/R plus one to two additional INSTI mutations.
References
Ref 1 Comparable In Vitro Activities of Second-Generation HIV-1 Integrase Strand Transfer Inhibitors (INSTIs) on HIV-1 Clinical Isolates with INSTI Resistance Mutations. Antimicrob Agents Chemother. 2019 Dec 20;64(1):e01717-19. doi: 10.1128/AAC.01717-19. Print 2019 Dec 20.

If you find any error in data or bug in web service, please kindly report it to Dr. Sun and Dr. Zhang.