Bictegravir

Bictegravir Properties

Melting point	>130°C (dec.)
Boiling point	682.5±55.0 °C(Predicted)
Density	1.62±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
solubility	DMSO (Slightly), Methanol (Slightly)
pka	4.50±1.00(Predicted)
form	Solid
color	White to Off-White
FDA UNII	8GB79LOJ07

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H315-H319-H335

Precautionary statements

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

NFPA 704

	0
2		0

Bictegravir price More Price(17)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	26532	Bictegravir	1611493-60-7	1mg	$26	2024-03-01	Buy
Cayman Chemical	26532	Bictegravir	1611493-60-7	10mg	$796	2023-06-20	Buy
Cayman Chemical	26532	Bictegravir	1611493-60-7	5mg	$65	2024-03-01	Buy
Cayman Chemical	26532	Bictegravir	1611493-60-7	25mg	$1873	2023-06-20	Buy
TRC	B382095	Bictegravir	1611493-60-7	1mg	$140	2021-12-16	Buy

Product number	Packaging	Price	Buy
26532	1mg	$26	Buy
26532	10mg	$796	Buy
26532	5mg	$65	Buy
26532	25mg	$1873	Buy
B382095	1mg	$140	Buy

Bictegravir Chemical Properties,Uses,Production

Description

Bictegravir (BIC) is a second-generation integrase strand transfer inhibitor (InSTI), like dolutegravir, with higher genetic barrier to resistance than raltegravir and elvitegravir.
Bictegravir is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor, the fourth in this class of agents that target the viral integrase. Bictegravir is used only in combination with other antiretroviral agents in the treatment of HIV infection and it has had limited use. Bictegravir is associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of acute, clinically apparent liver injury.

Uses

Bictegravir, is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

Definition

ChEBI: Bictegravir is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) and used (as its sodium salt) for the treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It is a monocarboxylic acid amide, a secondary carboxamide, a trifluorobenzene and an organic heterotetracyclic compound. It is a conjugate acid of a bictegravir(1-).

Application

Bictegravir, is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. Bictegravir is a recently approved investigational drug that has been used in trials studying the treatment of HIV-1 and HIV-2 infection. It has been approved for HIV-1 monotherapy combined with 2 other antiretrovirals in a single tablet. Bictegravir is indicated in the management of HIV-1 infection in patients not previously treated with antiretroviral therapy. Additionally, Bictegravir is indicated in the management of HIV-1 infection in patients who are virologically suppressed (HIV-1 RNA <50 c/mL) on a regular antiretroviral regimen for a minimum of three months without a history of failure in treatment and no known factors associated with the resistance to the individual components of the medication. It is used in combination with tenofovir and emtricitabine.

Mechanism of action

This single dose medication inhibits the strand transfer of viral DNA into the human genome, preventing HIV-1 virus replication and propagation 2.
In vitro, bictegravir has shown powerful antiviral activity against HIV-2 and various subtypes of HIV-1. It has shown synergistic effects when combined with other ARVs, including tenofovir alafenamide (TAF), emtricitabine (FTC), and darunavir (DRV) Label. The three components of the first USA approved medication ( trade name: Biktarvy ) are as follows:
Bictegravir: integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme necessary for viral replication. Inhibition of the integrase enzyme prevents the integration of HIV-1 into host DNA, blocking the conversion of the HIV-1 provirus and progression of the virus.
Emtricitabine: FTC, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine is phosphorylated to form emtricitabine 5'-triphosphate intracellularly. This metabolite inhibits the activity of human immunodeficiency virus (HIV) reverse transcriptase by competing with the substrate deoxycytidine 5'-triphosphate and by incorporating itself into viral DNA preventing DNA chain elongation.
Tenofovir Alafenamide: TAF is a phosphonamidate prodrug of tenofovir (2′-deoxyadenosine monophosphate analog). Plasma exposure to TAF leads to leakage into cells and then TAF is intracellularly converted to tenofovir by hydrolysis by cathepsin. Tenofovir is subsequently phosphorylated by cellular kinases to the metabolite tenofovir diphosphate, which is the active form of the drug. Tenofovir diphosphate inhibits HIV-1 replication by incorporating into viral DNA by the HIV reverse transcriptase, resulting in DNA chain-termination. Tenofovir diphosphate also weakly inhibits mammalian DNA polymerases.

Pharmacokinetics

Bictegravir is an HIV-1 integrase strand transfer inhibitor (INSTI). Bictegravir (BIC) inhibits HIV-1 virus replication into the human genome. It can be taken once daily without additional dosing. Bictegravir (BIC) inhibits strand transfer of viral DNA into the host genome and thereby prevents HIV-1 replication.

Side effects

Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or throat;
High lactic acid level—muscle pain or cramps, stomach pain, trouble breathing, general discomfort and fatigue;
Infection—fever, chills, cough, or sore throat;
Kidney injury—decrease in the amount of urine, swelling of the ankles, hands, or feet;
Liver injury—right upper belly pain, loss of appetite, nausea, light-colored stool, dark yellow or brown urine, yellowing skin or eyes, unusual weakness or fatigue;
Diarrhea, Headache, Nausea

Bictegravir synthesis

Synthesis of Bictegravir from (2R,5S,13aR)-8-methoxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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

Bictegravir Preparation Products And Raw materials

Raw materials

(2R,5S,13aR)-8-methoxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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

Preparation Products

Bictegravir Suppliers

Global( 162)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
BIONNA MEDICINE CO.,LTD	01056380788-8515; +8618518759099	790226113@qq.com	China	52	58
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Hangzhou ICH Biofarm Co., Ltd	+undefined8613073685410	sales@ichemie.com	China	985	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9348	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
TianYuan Pharmaceutical CO.,LTD	+86-755-23284190 13684996853	sales@tianpharm.com	CHINA	304	58
Jinan Carbotang Biotech Co.,Ltd.	+8615866703830	figo.gao@foxmail.com	China	6992	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58

Supplier	Advantage
BIONNA MEDICINE CO.,LTD	58
shandong perfect biotechnology co.ltd	58
Hangzhou ICH Biofarm Co., Ltd	58
Henan Tianfu Chemical Co.,Ltd.	55
Hangzhou FandaChem Co.,Ltd.	55
career henan chemical co	58
TianYuan Pharmaceutical CO.,LTD	58
Jinan Carbotang Biotech Co.,Ltd.	58
BOC Sciences	58
Chongqing Chemdad Co., Ltd	58

View Lastest Price from Bictegravir manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2024-03-12	Bictegravir 1611493-60-7	US $0.00 / g	1g	98% HPLC	1kg	shandong perfect biotechnology co.ltd
2023-11-27	Bictegravir 1611493-60-7	US $0.00-0.00 / kg	1kg	99%	500kg	Wuhan Senwayer Century Chemical Co.,Ltd
2023-11-01	Bictegravir 1611493-60-7	US $0.00-0.00 / kg	1kg	99.0%	20 tons	Hangzhou ICH Biofarm Co., Ltd

Bictegravir
1611493-60-7
US $0.00 / g
98% HPLC
shandong perfect biotechnology co.ltd

Bictegravir
1611493-60-7
US $0.00-0.00 / kg
99%
Wuhan Senwayer Century Chemical Co.,Ltd

Bictegravir
1611493-60-7
US $0.00-0.00 / kg
99.0%
Hangzhou ICH Biofarm Co., Ltd

Bictegravir Spectrum

Bictegravir(1611493-60-7)¹HNMR

1611493-60-7(Bictegravir)Related Search:

(1R,3S)-3-Aminocyclopentanol (1S,3R)-3-Aminocyclopentanol (2R,5S,13aR)-8-methoxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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 Salmeterol 1-(4-Acetyloxy)-3-((acetyloxy)methyl)phenyl)-2-bromoethanone

5-(2R)-2-Oxiranyl-8-benzyloxy-2(1H)-quinolinone (2R,5S,13aR)-8-methoxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid 1-(2,2-diMethoxyethyl)-5-Methoxy-6-(Methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid GSK1349572 2-BROMO-1-[4-HYDROXY-3-(HYDROXYMETHYL)PHENYL]ETHAN-1-ONE

O-Methyl Dolutegravir 4-Acetoxy-3-acetoxymethylacetophenone (6a,11b,16a,17a)-6,9-Difluoro-11,17-dihydroxy-16-methyl-3-oxoandrosta-1,4-diene-17-carboxylic acid (4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid N-(2-Chloropyrimidin-4-YL)-2,3-dimethyl-2H-indazol-6-amine

N-(2-chloropyriMidin-4-yl)-N,2,3-triMethyl-2H-indazol-6-aMine

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Bictegravir GS-9883 (2R,5S,13aR)-2,3,4,5,7,9,13,13a-Octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide Bictegravir (GS-9883) (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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 BNKY010-BC03 BICTEGRAVIR;GS-9883;GS 9883;GS9883 (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl) 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]-, (2R,5S,13aR)- Bictegravin Bictegravir (100 mg/mL in DMSO) BICTEGRAVIR-D5 Bitravir GS-9883-01 (2R,5S,13aR)-8-Hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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 1611493-60-7 161493-60-7 C21H18F3N3O5 Pharmaceutical