Tofacitinib citrate

Tofacitinib citrate 속성

Tofacitinib citrate C화학적 특성, 용도, 생산

개요

Tofacitinib citrate, also known as CP-690550 citrate, is a king of drugs developed by the US pharmaceutical company Pfizer for treating rheumatoid arthritis, trade name Xeljanz, for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid arthritis (RA) in adult patients. This product is a Janus kinase inhibitor, administered twice daily.
November 6, 2012, the US Food and Drug Administration (FDA) and Pfizer jointly announced Tofacitinib citrate is approved for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid joints arthritis (RA) in adult patients.
Xeljanz can be used as monotherapy or in combination with methotrexate or other non-biological disease-modifying antirheumatic drugs (the DMARD) in combination. This medicine should not be in combination with biological DMARD or strong immunosuppressants (such as cyclosporine and azathioprine). Xeljanz is approved by the daily dose of 2 times, each time 5mg.
Seven clinical trials evaluated the safety and efficacy of Tofacitinib citrate in moderate to severe active RA in adult patients. In all tests, compared with patients receiving placebo, patients receiving Xeljanz treatment showed significant improvement in clinical response and physical function.
In Clinical trials, the most common adverse events were upper respiratory tract infection, headache, diarrhea, nasal congestion, sore throat, and nasopharyngitis.
Using Xeljanz was associated with an increased risk of serious infections, including opportunistic infections, tuberculosis, cancer and lymphoma. Xeljanz product label attaches boxed warning on these security risks. Xeljanz treatment is also associated with reducing blood cell counts and increasing cholesterol and liver enzyme values.
In order to study Xeljanz long-term impact on heart disease, cancer and severe infections, FDA requires for a post-marketing study, which will evaluate two doses of Xeljanz (Tofacitinib citrate) therapy, and accept a integration of another group of patients approved by the treatment as a control.

용도

Tofacitinib citrate has been used:
as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studies
as a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan loss
as a Janus kinase inhibitor in MCF7 breast cancer cells

정의

ChEBI: Tofacitinib citrate is a citrate salt obtained by combining equimolar amounts of tofacitinib and citric acid. Used to treat moderately to severely active Rheumatoid Arthritis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antirheumatic drug. It contains a tofacitinib.

일반 설명

Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.

신진 대사

70% metabolised in the liver by CYP3A4 (major) and CYP2C19 (minor). The 8 metabolites produced are inactive.

참고 문헌

1. The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis. PMID: 26966791
2. Binding of Janus kinase inhibitor tofacitinib with human serum albumin: multi-technique approach DOI:10.1080/07391102.2015.1104522
3. Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo. DOI:10.1016/j.bcp.2018.07.034
4. Phosphoproteome profiling reveals critical role of JAK-STAT signaling in maintaining chemoresistance in breast cancer DOI:10.18632/oncotarget.21801
5. Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34 DOI:10.1016/j.tips.2010.10.004
6. http://www.medicinenet.com/tofacitinib_citrate_xeljanz/article.htm

Tofacitinib citrate 준비 용품 및 원자재

원자재

준비 용품

Tofacitinib citrate 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Senova Technology Co. Ltd.	+86-0755-86703119 +8618503098836	info@senovatech.com	China	349	58
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15377	58
Huadong Medicine (Xi'an)Bodyguard Pharmaceutical Co.,Ltd.	+86-029-86185165 +8618629664246	guoyuan@eastchinapharm.com	China	1615	58
Changsha Junyu Chemexpress.co., Ltd	+86-13723890100	info@csjyyy.cn	China	134	58
Changzhou Rokechem Technology Co., Ltd.	18758118018	sales001@rokechem.com	China	255	58
TAIZHOU YUXIN BIOTECHNOLOGY CO,.LTD	+86-576-88902229;+86-0576-88902229 +8613968687450	yuxin@yuxchem.com	China	122	58
Zibo Wei Bin Import & Export Trade Co. Ltd.	+86-0533-2091136 +8613864437655	ziboweibinmaoyi@163.com	China	100	58
Hebei Duling International Trade Co. LTD	+8618032673083	sales05@hbduling.cn	China	15747	58
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	7377	58

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