Apixaban
|
|
Apixaban ??
- ???
- 235-238°C
- ?? ?
- 770.5±60.0 °C(Predicted)
- ??
- 1.42
- ?? ??
- Refrigerator
- ???
- DMSO(?? ???, ??), ???(?? ???)
- ?? ?? (pKa)
- 15.01±0.20(Predicted)
- ??? ??
- ??
- ??? ??
- ??? ??
- ??
- ???? ?????
- InChI
- 1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)
- InChIKey
- QNZCBYKSOIHPEH-UHFFFAOYSA-N
- SMILES
- C1(=O)N(C2=CC=C(N3CCCCC3=O)C=C2)CCC2C(C(N)=O)=NN(C3=CC=C(OC)C=C3)C1=2
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| WGK ?? | WGK 3 | ||
|---|---|---|---|
| ???? ??? | 11 - Combustible Solids | ||
| ?? ?? ??? | 503612-47-3(Hazardous Substances Data) |
| ????(GHS): |
|
||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ?? ?: | Warning | ||||||||||||||
| ??·?? ??: |
|
||||||||||||||
| ??????: |
|
Apixaban C??? ??, ??, ??
??
Eliquis (apixaban), a direct inhibitor of factor Xa (FXa), was approved by the European Commission on May 18, 2011 for prevention of venous thromboembolic events (VTE) in adult patients who have undergone elective hip or knee replacement surgery. Apixaban (357.5 mg) also prevents thrombus formation without inducing adverse bleeding events in a porcine model of aortic heterotopic valve replacement. Formulations containing apixaban have been used to prevent blood clot formation in patients with atrial fibrillation.??
Apixaban is an oral anticoagulant jointly developed by Bristol-Myers Squibb (BMY) and Pfizer (PFE) for the prevention of stroke and systemic embolism in patients with atrial fibrillation. It is marketed under the brand name Eliquis. The drug was approved for use by the European Medicines Agency in 2011 and by the U.S. Food and Drug Administration in 2012.??
Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.??
ChEBI: A pyrazolopyridine that is 7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide substituted at position 1 by a 4-methoxyphenyl group and at position 6 by a 4-(2-oxopiperidin-1-yl)phenyl group. It is used for the prevention and treatment of thromboembolic diseases.Pharmacokinetics
The maximum plasma concentration (Cmax) of apixaban occurs 3–4 h after oral administration. The absorption of apixaban appears to occur primarily in the small intestine and decreases progressively throughout the gastrointestinal tract. Compared with oral administration, the bioavailability of 2.5 mg of apixaban solution was approximately 60% and 84% lower when released in the distal small bowel and ascending colon, respectively. For oral doses up to 10 mg, the absolute bioavailability of apixaban is~50%, resulting from the incomplete absorption and first-pass metabolism in the gut and liver[1].Clinical Use
Apixaban is an oral anticoagulant with highly selective inhibition of factor Xa. It was approved by the European Medicines Agency (EMA) for the treatment of venous thromboembolic events and first marketed in Germany under the brand name Eliquis in June 2011. Apixaban was co-developed by Bristol-Myers Squibb and Pfizer and represents the first approved drug for this indication since warfarin over 50 years ago.???
Possible side effects of Apixaban are: bleeding gums, nosebleeds, heavy vaginal bleeding , red, pink, or brown urine; red or black, tarry stools; coughing or spitting up blood or a substance that looks like coffee grounds; swelling or joint pain, headache, rash, chest pain or tightness in the chest, swelling of the face or tongue, trouble breathing, wheezing. Feeling dizzy or fainting.Apixaban prevents your blood from clotting properly, so if you get a cut or injury, it may take longer than usual for the bleeding to stop. This medication may also cause you to bruise or bleed more easily.?? ??
https://en.wikipedia.org/wiki/Apixabanhttps://www.drugbank.ca/drugs/DB06605
[1] Wonkyung Byon. “Apixaban: A Clinical Pharmacokinetic and Pharmacodynamic Review.” Clinical Pharmacokinetics 58 10 (2019): 1265–1279.
Apixaban ?? ?? ? ???
???
?? ??
Apixaban ?? ??
???( 942)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Linyi Changqing Chemical Co., LTD | +86-0532-55729510 +86-15853232676 |
marketing@echemi.com | China | 288 | 58 |
| Jinan Jianfeng Chemical Co., Ltd | +86-0531-88110457 +8615562555968 |
info@pharmachemm.com | China | 311 | 58 |
| AFINE CHEMICALS LIMITED | +86-571-85134551 |
info@afinechem.com | China | 15081 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 |
market18@leapchem.com | China | 43333 | 58 |
| Hangzhou Hyper Chemicals Limited | +86-0086-57187702781 +8613675893055 |
info@hyper-chem.com | China | 310 | 58 |
| S&Y Biochem Co.,Ltd | +86-17774091612; +8617774091612 |
marketing@sybiochem.com | China | 284 | 58 |
| Jinan Million Pharmaceutical Co., Ltd | 0531-68659554 +8613031714605 |
info@millionpharm.com | China | 184 | 58 |
| Yiwu Fengjin Commercial Company | +undefined-86-19164429943 +undefined19164429943 |
jaspercc0416@163.com | China | 1000 | 58 |
| Hebei Chuanghai Biotechnology Co., Ltd | +8615350571055 |
Sibel@chuanghaibio.com | China | 8738 | 58 |
| Hebei Yanxi Chemical Co., Ltd. | +8618531123677 |
faithe@yan-xi.com | China | 5853 | 58 |
Apixaban ?? ??:
Voriconazole
Apixaban IMpurity(BMS-591329-01)
5-chloro-N-(4-(5-morpholino-6-oxo-3,6-dihydropyridin-1(2H)-yl)phenyl)pentanamide
Apixaban IMpurity(
1,3-bis(4-bromophenyl)propan-2-one
3-Chloro-1-(4-nitrophenyl)-5,6-dihydropyridin-2(1H)-one
3-Morpholino-1-(4-(2-oxopiperidin-1-yl)phenyl)-5,6-dihydropyridin-2(1H)-one
Apixaban IMpurity 6
1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester
Rivaroxaban
Bortezomib
MK-2206 2HCl
Dabigatran
Ethyl (2Z)-chloro[(4-methoxyphenyl)hydrazono]ethanoate
Edoxaban tosylate monohydrate
(+)-JQ-1
1-(4-Methoxyphenyl)-6-(4-(2-Methyl-6-oxopiperidin-1-yl)phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxaMide
Apixaban IMpurity 5 (BMS-591329-01)