パゾパニブ
WordNet
- the writing point of a pen (同)pen nib
PrepTutorEJDIC
- ペン先 / (一般的に)とがった部分,先端(tip) / (鳥の)くちばし
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/08/11 17:44:57」(JST)
[Wiki en表示]
Pazopanib
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Systematic (IUPAC) name |
5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzolsulfonamide |
Clinical data |
Trade names |
Votrient |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a610013 |
Licence data |
EMA:Link, US FDA:link |
Pregnancy cat. |
D (US) |
Legal status |
℞-only (US) |
Routes |
Oral |
Pharmacokinetic data |
Protein binding |
>99% |
Metabolism |
Hepatic (CYP3A4, 1A2 and 2C8-mediated) |
Half-life |
31 hours (mean) |
Excretion |
Mostly fecal |
Identifiers |
CAS number |
444731-52-6 N |
ATC code |
L01XE11 |
PubChem |
CID 11525740 |
ChemSpider |
9700526 Y |
UNII |
7RN5DR86CK Y |
ChEMBL |
CHEMBL477772 N |
Chemical data |
Formula |
C21H23N7O2S |
Mol. mass |
437.517 g/mol |
SMILES
- O=S(=O)(N)c1c(ccc(c1)Nc2nccc(n2)N(c4ccc3c(nn(c3C)C)c4)C)C
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InChI
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InChI=1S/C21H23N7O2S.ClH/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16;/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25);1H Y
Key:MQHIQUBXFFAOMK-UHFFFAOYSA-N Y
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N (what is this?) (verify)
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Pazopanib (trade name Votrient) is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by the U.S. Food and Drug Administration.[1][2][3] Pazopanib may also be active in ovarian cancer[4] Pazopanib also appears effective in the treatment of non-small cell lung carcinoma.[4]
References[edit source | edit]
- ^ "FDA Approves GlaxoSmithKline's Votrient(TM) For Advanced Renal Cell Cancer". Medical News Today. 20 October 2009. Retrieved 8 June 2010.
- ^ Sleijfer, S.; Ray-Coquard, I.; Papai, Z.; Le Cesne, A.; Scurr, M.; Schoffski, P.; Collin, F.; Pandite, L. et al. (2009). "Pazopanib, a Multikinase Angiogenesis Inhibitor, in Patients with Relapsed or Refractory Advanced Soft Tissue Sarcoma: A Phase II Study from the European Organisation for Research and Treatment of Cancer-Soft Tissue and Bone Sarcoma Group (EORTC Study 62043)". Journal of Clinical Oncology 27 (19): 3126. doi:10.1200/JCO.2008.21.3223. PMID 19451427. edit
- ^ "FDA Approves Glaxo Cancer Drug Votrient". Reuters. 26 April 2012. Retrieved 27 April 2012.
- ^ a b "Pazopanib shows encouraging activity in several tumour types, including soft tissue sarcoma and ovarian cancer". FierceBiotech. 2008-09-15. Retrieved 2010-08-10.
Targeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01)
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CI monoclonal antibodies ("-mab") |
Receptor tyrosine kinase
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- ErbB: HER1/EGFR (Cetuximab
- Panitumumab)
- HER2/neu (Trastuzumab
- Trastuzumab emtansine)
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Others for solid tumors
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- EpCAM (Catumaxomab
- Edrecolomab)
- VEGF-A (Bevacizumab)
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Leukemia/lymphoma
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- lymphoid: CD20 (Ibritumomab
- Ofatumumab
- Rituximab
- Tositumomab), CD30 (Brentuximab), CD52 (Alemtuzumab)
myeloid: CD33 (Gemtuzumab)
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Tyrosine-kinase inhibitors ("-nib") |
Receptor tyrosine kinase
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- ErbB: HER1/EGFR (Erlotinib
- Gefitinib
- Vandetanib)
- HER1/EGFR and HER2/neu (Afatinib
- Lapatinib
- Neratinib)
- RTK class III: C-kit and PDGFR (Axitinib
- Masitinib
- Pazopanib
- Sunitinib
- Sorafenib
- Toceranib)
- FLT3 (Lestaurtinib)
- VEGFR (Axitinib
- Cediranib
- Pazopanib
- Regorafenib
- Semaxanib
- Sorafenib
- Sunitinib
- Toceranib
- Vandetanib)
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Non-receptor
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- bcr-abl (Imatinib
- Dasatinib
- Nilotinib
- Ponatinib)
- Janus kinase (Lestaurtinib
- Ruxolitinib)
EML4-ALK (Crizotinib)
RET inhibitors: Vandetanib (Also VEGFR and EGFR).
c-MET inhibitor: Cabozantinib (Also VEGFR2).
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Other |
- fusion protein against VEGF (Aflibercept)
- proapoptotic peptide against ANXA2 and prohibitin (Adipotide)
- exotoxin against IL-2 (Denileukin diftitox)
- mTOR inhibitors (Everolimus
- Temsirolimus)
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UpToDate Contents
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English Journal
- Pruritus in patients treated with targeted cancer therapies: Systematic review and meta-analysis.
- Ensslin CJ, Rosen AC, Wu S, Lacouture ME.SourceDermatology Service, Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, New York.
- Journal of the American Academy of Dermatology.J Am Acad Dermatol.2013 Nov;69(5):708-20. doi: 10.1016/j.jaad.2013.06.038. Epub 2013 Aug 24.
- BACKGROUND: Pruritus has been anecdotally described in association with targeted cancer therapies. The risk of pruritus has not been systematically ascertained.OBJECTIVE: A systematic review and meta-analysis of the literature was conducted for axitinib, cetuximab, dasatinib, erlotinib, everolimus,
- PMID 23981682
- Small molecule targeted therapies for the second-line treatment for metastatic renal cell carcinoma: a systematic review and indirect comparison of safety and efficacy.
- Dranitsaris G, Schmitz S, Broom RJ.SourceUniversity of Ioannina, Ioannina, Greece, george.dranitsaris@gmail.com.
- Journal of cancer research and clinical oncology.J Cancer Res Clin Oncol.2013 Nov;139(11):1917-26. doi: 10.1007/s00432-013-1510-5. Epub 2013 Sep 14.
- BACKGROUND: Patients with metastatic renal cell carcinoma (mRCC) and a good performance status typically receive an anti-vascular endothelial growth factor receptor (VEGFR) TKI (sunitinib or pazopanib) as initial therapy. Upon disease progression or intolerance, there are four orally administered ag
- PMID 24037486
- A validated assay for the simultaneous quantification of six tyrosine kinase inhibitors and two active metabolites in human serum using liquid chromatography coupled with tandem mass spectrometry.
- van Erp NP, de Wit D, Guchelaar HJ, Gelderblom H, Hessing TJ, Hartigh Jd.SourceDepartment of Clinical Pharmacy & Toxicology, Leiden University Medical Center, Leiden, The Netherlands; Department of Clinical Pharmacy, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands. Electronic address: P.vanErp@akf.umcn.nl.
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.J Chromatogr B Analyt Technol Biomed Life Sci.2013 Oct 15;937:33-43. doi: 10.1016/j.jchromb.2013.08.013. Epub 2013 Aug 17.
- A sensitive, sophisticated and practical bioanalytical assay for the simultaneous determination of six tyrosine kinase inhibitors (imatinib, sunitinib, nilotinib, dasatinib, pazopanib, regorafenib) and two active metabolites (N-desmethyl imatinib and N-desethyl sunitinib) was developed and validated
- PMID 24013127
Japanese Journal
- 経験と考察 進行性軟部肉腫に対するパゾパニブ塩酸塩の治療効果と有害事象
- 鈴木 賀代,安田 剛敏,渡邉 健太 [他]
- 整形外科 = Orthopedic surgery 66(5), 418-422, 2015-05
- NAID 40020456323
- 後腹膜脂肪肉腫再発3例に対するパゾパニブの使用経験
- 小泉 淳,井上 高光,高山 孝一朗 [他],高橋 誠,沼倉 一幸,鶴田 大,秋濱 晋,齋藤 満,成田 伸太郎,土谷 順彦,佐藤 滋,羽渕 友則
- 泌尿器科紀要 = Acta urologica Japonica 61(4), 153-158, 2015-04
- … Pazopanib, a novel tyrosine kinase inhibitor, is an effective therapeutic agent for patients with advanced soft tissue sarcoma. … Here we report three patients with recurrent retroperitoneal liposarcoma who were treated with pazopanib. … Because of the lack of response to chemotherapy, 400 mg/day of pazopanib was subsequently administered for two weeks. … Pazopanib (600 mg/day) was partially effective for 2 months. …
- NAID 120005611425
- Primary Pleural Synovial Sarcoma Treated with Pazopanib
- Sugitani Arata,Asai Kazuhisa,Kojima Kazuya,Eguchi Yosuke,Kawaguchi Tomoya,Ohsawa Masahiko,Hirata Kazuto
- Internal Medicine 54(16), 2051-2055, 2015
- … Although treated with pazopanib as second-line chemotherapy, the patient died eight months after the initial presentation. …
- NAID 130005092891
Related Links
- 米食品医薬品局(FDA)は、2012年4月26日、英GlaxoSmithKline社(GSK社)が申請していた、化学療法歴のある進行悪性軟部腫瘍患者への「Votrient」(一般名pazopanib;パゾパニブ)の適用を承認したと発表した。 pazopanibは経口 ...
- GlaxoSmithKline Official Website, グラクソ・スミスクライン株式会社公式ウェブサイト ... グラクソ・スミスクラインの抗がん剤Pazopanib、 進行性の腎細胞がん、卵巣がん、軟部肉腫に効果を示す 2007-06-15
Related Pictures
★リンクテーブル★
[★]
nib
[★]
- 英
- motesanib
- 開発名
- AMG706
文献
- Efficacy and safety of motesanib, an oral inhibitor of VEGF, PDGF, and Kit receptors, in patients with imatinib-resistant gastrointestinal stromal tumors.
- Cancer Chemother Pharmacol. 2010 Sep 14. [Epub ahead of print]
- Benjamin RS, Schoffski P, Hartmann JT, Van Oosterom A, Bui BN, Duyster J, Schuetze S, Blay JY, Reichardt P, Rosen LS, Skubitz K, McCoy S, Sun YN, Stepan DE, Baker L.
- PMID 20838998
参考
- http://www.mikanbox.com/md-lab/column/imashuku/Column6/column6_25.html
[★]
- 英
- pazopanib
- 商
- ヴォトリエント
- 化
- パゾパニブ塩酸塩 pazopanib hydrochloride