BICTEGRAVIR SODIUM

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H17F3N3O5.Na
Molecular Weight	471.3618
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[Na+].[H][C@@]12CN3C=C(C(=O)NCC4=C(F)C=C(F)C=C4F)C(=O)C([O-])=C3C(=O)N1[C@H]5CC[C@H](C5)O2

InChI

InChIKey=WJNFBIVCQMPPJC-FQYDJHLKSA-M

InChI=1S/C21H18F3N3O5.Na/c22-9-3-14(23)12(15(24)4-9)6-25-20(30)13-7-26-8-16-27(10-1-2-11(5-10)32-16)21(31)17(26)19(29)18(13)28;/h3-4,7,10-11,16,29H,1-2,5-6,8H2,(H,25,30);/q;+1/p-1/t10-,11+,16+;/m0./s1

HIDE SMILES / InChI

Molecular Formula	Na
Molecular Weight	22.9898
Charge	1
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C21H17F3N3O5
Molecular Weight	448.372
Charge	-1
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/27645238

Bictegravir is a component of the fixed-dose combination product bictegravir/emtricitabine/tenofovir alafenamide (BIKTARVY®), which received marketing approval for the treatment of human immunodeficiency virus (HIV) infection by the U.S. Food and Drug Administration in February 2018. Bictegravir inhibits the strand transfer activity of HIV-1 integrase, 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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Human immunodeficiency virus type 1 integrase 19 Target ID: CHEMBL3471 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	Inhibitor 8297		7.5 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
HIV-1 infection 151 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	Primary		Approved 8429	BIKTARVY Approved Use BIKTARVY is a three-drug combination of bictegravir (BIC), a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI), and emtricitabine (FTC) and tenofovir alafenamide (TAF), both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs), and is indicated as a complete regimen for the treatment of HIV-1 infection in adults 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 for at least 3 months with no history of treatment failure and no known substitutions associated with resistance to the individual components of BIKTARVY. Launch Date 1.48633918E12

C_max

Value	Dose	Co-administered	Analyte	Population
12235 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
3475 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
6080 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
741.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
6.15 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: EMTRICITABINE	EMTRICITABINE	BICTEGRAVIR SODIUM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
178901.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
48950.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
87538.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9983 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
102 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: EMTRICITABINE	EMTRICITABINE	BICTEGRAVIR SODIUM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
20.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
15.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
17.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28196003/	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BICTEGRAVIR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
17.3 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: EMTRICITABINE	EMTRICITABINE	BICTEGRAVIR SODIUM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: EMTRICITABINE	EMTRICITABINE	BICTEGRAVIR SODIUM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	Other AEs: Diarrhea, Nausea... Other AEs: Diarrhea (all grades, 6%) Nausea (all grades, 5%) Headache (all grades, 5%) Fatigue (all grades, 3%) Abnormal dreams (all grades, 3%) Dizziness (all grades, 2%) Insomnia (all grades, 2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8	Other AEs: Amylase, ALT... Other AEs: Amylase (grade 3-4, 2%) ALT (grade 3-4, 1%) Neutrophils (grade 3-4, 2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8

AEs

AE	Significance	Dose	Population
Dizziness	all grades, 2%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Insomnia	all grades, 2%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Abnormal dreams	all grades, 3%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Fatigue	all grades, 3%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Headache	all grades, 5%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Nausea	all grades, 5%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
Diarrhea	all grades, 6%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 7
ALT	grade 3-4, 1%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8
Amylase	grade 3-4, 2%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8
Neutrophils	grade 3-4, 2%	50 mg 1 times / day multiple, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8	unhealthy, adult n = 314 Health Status: unhealthy Condition: HIV-1 Age Group: adult Sex: unknown Population Size: 314 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf Page: 8

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT2 647 MATE1 306 OATP1B1 788 OATP1B3 706 OCT1 512 BSEP 402 OAT1 599 OAT3 642 UGT1A1 204 CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP3A 214	UGT1A1 418 P-gp 1537 BCRP 561	CYP3A 129

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
UGT1A1 254	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 410	no [IC50 176 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419, 430	no [IC50 >100 uM]
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419, 430	no [IC50 >100 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419, 430	no [IC50 >100 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419, 430	no [IC50 >100 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419, 430	no [IC50 >100 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 407.0	no [IC50 >100 uM]
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 430	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 430	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 430	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 430	no
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 430	no
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 407, 419	weak [IC50 >100 uM]
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67	weak
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 62, 66, 430	yes [IC50 0.42 uM]	likely (co-administration study) Comment: coadministration of BIKTARVY with drugs that are substrates of OCT2 may increase their plamsa concentrations Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 62, 66, 430
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 62, 67, 430	yes [IC50 8.04 uM]	likely (co-administration study) Comment: coadministration of BIKTARVY with drugs that are substrates of MATE1 may increase their plamsa concentrations Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 62, 67, 430

Drug as victim

Target	Modality	Activity	Clinical evidence
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66.0	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67	yes	yes (co-administration study) Comment: rifampin decreased the mean bictegravir Cmax by 28% and AUC by 75%; rifbutin decreased the mean bictegravir Cmax by 20% and AUC by 38% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67	yes	yes (co-administration study) Comment: rifampin decreased the mean bictegravir Cmax by 28% and AUC by 75%; rifbutin decreased the mean bictegravir Cmax by 20% and AUC by 38% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67
UGT1A1 418	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67	yes	yes (co-administration study) Comment: rifampin decreased the mean bictegravir Cmax by 28% and AUC by 75% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 66, 67

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf Page: 40, 42-43

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA01EN1S	https://www.aablocks.com/goods/Goods/detail?id=AA01EN1S
Aaron Chemicals	AR01ENTK	http://www.aaronchem.com/1611493-60-7
AbMole Bioscience	M9113	http://www.abmole.com/products/bictegravir.html
Ambeed	A363683	https://www.ambeed.com/products/1611493-60-7.html
BLD Pharm	BD767657	http://www.bldpharm.com/products/1611493-60-7.html
BioChemPartner	BCP25703	http://www.biochempartner.com/1611493-60-7-BCP25703
CSNpharm	CSN20343	https://www.csnpharm.com/products/bictegravir.html
Chem Scene	CS-0014685	http://www.chemscene.com/1611493-60-7.html
Chemspace	CSSB00103150645	https://chem-space.com/CSSB00103150645
DC Chemicals	DC10890	http://www.dcchemicals.com/product_show-Bictegravir.html
Excenen	EX-A3161	https://www.excenen.com/searchresultlist.php?id=1611493-60-7
MedChem Express	HY-17605	https://www.medchemexpress.com/Bictegravir.html
Selleck Chemicals	S5911	http://www.selleckchem.com/products/bictegravir.html
Smolecule	S521202	http://www.smolecule.com/products/s521202
Synblock Inc	SB18851	http://www.synblock.com/product/1611493-60-7.html
THE BioTek	bt-262052	https://www.thebiotek.com/product/inhibitors/bt-262052
eNovation Chemicals	D676014	https://www.enovationchem.com/ProductDetails.asp?ProductID=D676014
eNovation Chemicals	D763132	https://www.enovationchem.com/ProductDetails.asp?ProductID=D763132

PubMed

Title	Date	PubMed
Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.	2016 Dec	27645238
Antiviral Activity, Safety, and Pharmacokinetics of Bictegravir as 10-Day Monotherapy in HIV-1-Infected Adults.	2017 May 1	28196003
Bictegravir: First Global Approval.	2018 Apr	29564777

Patents

Sample Use Guides

In Vivo Use Guide

BIKTARVY® is a three-drug fixed dose combination product containing 50 mg of bictegravir, 200 mg of emtricitabine, and 25 mg of tenofovir alafenamide. The recommended dosage of BIKTARVY is one tablet taken orally once daily with or without food.

Route of Administration: Oral

In Vitro Use Guide

The antiviral activity of bictegravir (BIC) against laboratory and clinical isolates of HIV-1 was assessed in lymphoblastoid cell lines, PBMCs, primary monocyte/macrophage cells, and CD4+ T-lymphocytes. In MT-4 cells (human lymphoblastoid T-cell line) acutely infected with HIV-1 IIIB, the mean 50% effective concentration (EC50) was 2.4+/-0.4 nM, and the protein-adjusted EC95 value was 361 nM (0.162 micrograms per mL). BIC displayed antiviral activity in activated PBMCs against clinical isolates of HIV-1 representing groups M, N, and O, including subtypes A, B, C, D, E, F, and G, with a median EC50 value of 0.55 nM (range <0.05 to 1.71 nM). The EC50 value against a single HIV-2 isolate was 1.1 nM.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 08:41:33 UTC 2023` Edited by `admin` on `Sat Dec 16 08:41:33 UTC 2023`
Record UNII	4L5MP1Y7W7
Record Status	`Validated (UNII)`
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Name

Type

Language

BICTEGRAVIR SODIUM

Official Name

English

BICTEGRAVIR SODIUM [JAN]

Common Name

English

BICTEGRAVIR SODIUM [USAN]

Common Name

English

BICTEGRAVIR SODIUM [MI]

Common Name

English

BICTEGRAVIR SODIUM [ORANGE BOOK]

Common Name

English

BICTEGRAVIR SODIUM COMPONENT OF BIKTARVY

Common Name

English

GS-9883-01 SODIUM

Code

English

GS-9883 SODIUM

Code

English

BIKTARVY COMPONENT BICTEGRAVIR SODIUM

Brand Name

English

2,5-METHANOPYRIDO(1',2':4,5)PYRAZINO(2,1-B)(1,3)OXAZEPINE-10-CARBOXAMIDE, 2,3,4,5,7,9,13,13A-OCTAHYDRO-8-HYDROXY-7,9-DIOXO-N-((2,4,6-TRIFLUOROPHENYL)METHYL)-, SODIUM SALT (1:1), (2R,5S,13AR)-

Systematic Name

English

Bictegravir sodium [WHO-DD]

Common Name

English

(2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-((2,4,6-TRIFLUOROPHENYL)METHYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO(1',2':4,5)PYRAZINO(2,1-B)(1,3)OXAZEPINE-10-CARBOXAMIDE MONOSODIUM SALT

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1660