AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
bictegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 5274 | 1611493-60-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Bictegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.10 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | GRK2,PDK1,PDK2,PDK4 | 4 | |||
| kinase-selectivity-class | PDK1 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 21, 2018 | EMA | Gilead Sciences International Limited | |
| Feb. 7, 2018 | FDA | GILEAD SCIENCES INC | |
| March 26, 2019 | PMDA | Gilead Sciences K.K. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AR20 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
| CHEBI has role | CHEBI:67268 | HIV-1 integrase inhibitor |
Related Drugs by ATC class:
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.24 | acidic |
| pKa2 | 12.47 | acidic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | 8754065 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | 9296769 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | 8754065 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | 9296769 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | 10385067 | June 19, 2035 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | 10385067 | June 19, 2035 | TREATMENT OF HIV INFECTION |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | 12594244 | Nov. 8, 2036 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | 12594244 | Nov. 8, 2036 | TREATMENT OF HIV INFECTION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | June 18, 2026 | FOR HIV-1 INFECTION IN PEDIATRIC PTS AT LEAST 25 KG W/ NO ANTIRETROVIRAL (ARV) TX HX OR TO REPLACE CURRENT ARV REGIMEN FOR VIROLOGICALLY-SUPPRESSED ON STABLE ARV W/ NO HX TX FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED W/ RESISTANCE TO BIC, FTC, OR TAF |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | Feb. 23, 2027 | EXPANSION OF INDICATION TO USE OF BICTEGRAVIR/EMTRICITABINE/TENOFOVIR ALAFENAMIDE FOR THE TREATMENT OF HIV-1 INFECTION IN VIROLOGICALLY SUPPRESSED ADULTS AND PEDIATRIC PATIENTS ON A STABLE HIV-1 TREATMENT REGIMEN WITH NO KNOWN RESISTANCE TO BICTEGRAVIR OR TENOFOVIR |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | Feb. 23, 2027 | EXPANSION OF INDICATION TO USE OF BICTEGRAVIR/EMTRICITABINE/TENOFOVIR ALAFENAMIDE FOR THE TREATMENT OF HIV-1 INFECTION IN VIROLOGICALLY SUPPRESSED ADULTS AND PEDIATRIC PATIENTS ON A STABLE HIV-1 TREATMENT REGIMEN WITH NO KNOWN RESISTANCE TO BICTEGRAVIR OR TENOFOVIR |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | April 24, 2027 | REVISIONS TO THE LABELING TO INCLUDE INFORMATION FOR PREGNANT INDIVIDUALS |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | Oct. 7, 2028 | A COMPLETE REGIMEN FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTS WEIGHING 14 KG TO LESS THAN 25 KG WHO HAVE NO ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY-SUPPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INDIVIDUAL COMPONENTS OF BIKTARVY |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | Feb. 23, 2031 | TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 14 KG TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO BICTEGRAVIR OR TENOFOVIR AND WITH KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO EMTRICITABINE |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | Feb. 23, 2031 | TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 14 KG TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO BICTEGRAVIR OR TENOFOVIR AND WITH KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO EMTRICITABINE |
| EQ 30MG BASE;120MG;EQ 15MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Oct. 7, 2021 | RX | TABLET | ORAL | July 30, 2032 | TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTSWEIGHING AT LEAST 14 KG WITH AN ANTIRETROVIRAL TREATMENT HISTORY AND NOT VIROLOGICALLY SUPPRESSED, WITH NO KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INTEGRASE STRAND INHIBITOR CLASS, EMTRICITABINE, OR TENOFOVIR |
| EQ 50MG BASE;200MG;EQ 25MG BASE | BIKTARVY | GILEAD SCIENCES INC | N210251 | Feb. 7, 2018 | RX | TABLET | ORAL | July 30, 2032 | TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTSWEIGHING AT LEAST 14 KG WITH AN ANTIRETROVIRAL TREATMENT HISTORY AND NOT VIROLOGICALLY SUPPRESSED, WITH NO KNOWN OR SUSPECTED SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INTEGRASE STRAND INHIBITOR CLASS, EMTRICITABINE, OR TENOFOVIR |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Solute carrier family 22 member 2 | Transporter | IC50 | 6.31 | CHEMBL | |||||
| Integrase | Enzyme | INHIBITOR | IC50 | 8.13 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Integrase | Enzyme | IC50 | 8.12 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 8GB79LOJ07 | UNII |
| 1807988-02-8 | SECONDARY_CAS_RN |
| 4037318 | VANDF |
| C4507568 | UMLSCUI |
| CHEBI:172943 | CHEBI |
| KLQ | PDB_CHEM_ID |
| CHEMBL3989866 | ChEMBL_ID |
| 90311989 | PUBCHEM_CID |
| DB11799 | DRUGBANK_ID |
| CHEMBL3989867 | ChEMBL_ID |
| D10909 | KEGG_DRUG |
| 10133 | INN_ID |
| C000620396 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11575 | IUPHAR_LIGAND_ID |
| 772193003 | SNOMEDCT_US |
| 772194009 | SNOMEDCT_US |
| 816103009 | SNOMEDCT_US |
| 33694 | MMSL |
| d08735 | MMSL |
| 017460 | NDDF |
| 017461 | NDDF |
| 1999660 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Biktarvy | HUMAN PRESCRIPTION DRUG LABEL | 3 | 50090-6247 | TABLET | 50 mg | ORAL | NDA | 34 sections |
| Biktarvy | HUMAN PRESCRIPTION DRUG LABEL | 3 | 61958-2501 | TABLET | 50 mg | ORAL | NDA | 35 sections |
| Biktarvy | HUMAN PRESCRIPTION DRUG LABEL | 3 | 61958-2505 | TABLET | 30 mg | ORAL | NDA | 35 sections |
| Biktarvy | HUMAN PRESCRIPTION DRUG LABEL | 3 | 61958-2506 | TABLET | 30 mg | ORAL | NDA | 35 sections |