tipifarnib

WordNet

1. the writing point of a pen (同)pen nib

PrepTutorEJDIC

1. 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）』「2015/10/24 12:43:18」(JST)

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[Wiki en表示]

Tipifarnib

Systematic (IUPAC) name
6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
Identifiers
CAS Registry Number	Y
ATC code	None
PubChem	CID: 148193
UNII	MAT637500A N
ChEMBL	CHEMBL289228 N
Chemical data
Formula	C27H22Cl2N4O
Molecular mass	489.395 g/mol
N (what is this?)  (verify)

Tipifarnib (trade name Zarnestra) is a farnesyltransferase inhibitor that is being investigated in patients 65 years of age and older with newly diagnosed acute myeloid leukemia (AML). It inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive. It inhibits prenylation of the CxxX tail motif, which allows Ras to bind to the membrane where it is active. Without this step the protein cannot function.

It is also being tested in clinical trials in patients in certain stages of breast cancer.

For treatment of progressive plexiform neurofibromas associated with Neurofibromatosis type I, it successfully passed phase one clinical trials but was suspended (NCT00029354) in phase two. The compound was discovered by and is under investigation by Johnson & Johnson Pharmaceutical Research & Development, L.L.C, with registration number R115777.

Approval process

Tipifarnib was submitted to the FDA by Johnson & Johnson for the treatment of AML in patients aged 65 and over with a New Drug Application (NDA) to the Food and Drug Administration (FDA) on January 24, 2005.

In June 2005, the FDA issued a "not approvable" letter for tipifarnib.

References

Confocal microscopy photographs of the descending aortas of two 15-month-old progeria mice, one untreated (left picture) and the other treated with the farnsyltransferase inhibitor drug tipifarnib (right picture). The microphotographs show prevention of the vascular smooth muscle cell loss that is otherwise rampant by this age. Staining was smooth muscle alpha-actin (green), lamins A/C (red) and DAPI (blue). (Original magnification, x 40)

UpToDate Contents

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• 1. 再発性または難治性の急性骨髄性白血病の治療 treatment of relapsed or refractory acute myeloid leukemia
• 2. 甲状腺髄様癌：化学療法および免疫療法 medullary thyroid cancer chemotherapy and immunotherapy
• 3. 神経線維腫症I型（NF1）：マネージメントおよび予後 neurofibromatosis type 1 nf1 management and prognosis
• 4. 限局進行性および切除可能境界膵外分泌癌に対する初回化学療法および放射線治療 initial chemotherapy and radiation for nonmetastatic locally advanced unresectable borderline resectable and potentially resectable exocrine pancreatic cancer
• 5. ナチュラルキラー（NK）細胞大顆粒リンパ球性白血病 natural killer nk cell large granular lymphocyte leukemia

English Journal

• K-Ras and its inhibitors towards personalized cancer treatment: Pharmacological and structural perspectives.

• Asati V1, Mahapatra DK2, Bharti SK3.
• European journal of medicinal chemistry.Eur J Med Chem.2017 Jan 5;125:299-314. doi: 10.1016/j.ejmech.2016.09.049. Epub 2016 Sep 16.
• The discovery of genetic, genomic and clinical biomarkers have revolutionized the treatment option in the form of personalized medicine which allows to accurately predict a person's susceptibility/progression of disease, the patient's response to therapy, and maximize the therapeutic outcome in term
• PMID 27688185

• Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1α and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.

• Tanaka T1, Ikegami Y1, Nakazawa H1,2, Kuriyama N1,2, Oki M3, Hanai J3, Sukhatme VP3, Kaneki M4,5.
• Journal of cellular physiology.J Cell Physiol.2017 Jan;232(1):192-201. doi: 10.1002/jcp.25411. Epub 2016 Jun 15.
• The aggressiveness of triple-negative breast cancer (TNBC), which lacks estrogen receptor, progesterone receptor and epidermal growth factor receptor 2 (HER2), represents a major challenge in breast cancer. Migratory and self-renewal capabilities are integral components of invasion, metastasis and r
• PMID 27137755

• Phase II trial of pegylated interferon alfa-2b in young patients with neurofibromatosis type 1 and unresectable plexiform neurofibromas.

• Jakacki RI1, Dombi E2, Steinberg SM2, Goldman S2, Kieran MW2, Ullrich NJ2, Pollack IF2, Goodwin A2, Manley PE2, Fangusaro J1, Allen R2, Widemann BC2.
• Neuro-oncology.Neuro Oncol.2016 Aug 10. pii: now158. [Epub ahead of print]
• BACKGROUND: There is no proven medical therapy for plexiform neurofibromas (PNs). We undertook a phase II trial of pegylated interferon (PI) to evaluate response and time to progression (TTP).METHODS: PI was administered as a subcutaneous injection to patients with neurofibromatosis type 1‒related
• PMID 27510726

Japanese Journal

• Hutchinson-Gilford Progeria Syndrome : Its Presentation in F. Scott Fitzgerald's Short Story 'The Curious Case of Benjamin Button' and Its Oral Manifestations

• MALONEY W. J.
• Journal of dental research 88(10), 873-876, 2009-10-01
• NAID 10027305871

• Phase II trial of tipifarnib in patients with recurrent malignant glioma either receiving or not receiving enzyme-inducing antiepileptic drugs : a North American Brain Tumor Consortium Study

• CLOUGHESY T. F.
• J. Clin. Oncol. 24, 3651-3656, 2006
• NAID 30022792292

Related Pictures

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★リンクテーブル★

リンク元	「nib」「上皮成長因子受容体阻害薬」

「nib」

　　[★]

• 受容体のリガンド結合部を標的とした小分子化合物。

nib

• アキシチニブ axitinib
• ボスチニブ bosutinib
• ブリバニブ brivanib
• カネルチニブ canertinib
• セジラニブ cediranib
• ダサチニブ dasatinib　チロシンキナーゼ阻害薬　イマチニブ抵抗性の慢性骨髄性白血病、再発又は難治性のフィラデルフィア染色体陽性急性リンパ性白血病
• エルロチニブ erlotinib
• ゲフィチニブ gefitinib
• イマチニブ imatinib　チロシンキナーゼ阻害薬　CML、CKIT(CD117)陽性消化管間質腫瘍、
• ラパチニブ lapatinib
• レスタウルチニブ lestaurtinib
• リニファニブ linifanib
• ロナファーニブ lonafarnib
• ネラチニブ neratinib
• ニブリン nibrin
• ニロチニブ nilotinib　チロシンキナーゼ阻害薬　イマチニブ抵抗性の慢性期又は移行期の慢性骨髄性白血病
• パゾパニブ pazopanib
• ペガプタニブ pegaptanib
• ラニビズマブ ranibizumab
• セマキシニブ semaxinib
• ソラフェニブ sorafenib
• スニチニブ sunitinib　VEGFRやPDGFRチロシンキナーゼ阻害薬　イマチニブ抵抗性の消化管間質腫瘍、根治切除不能又は転移性の腎細胞癌
• ティピファニブ tipifarnib
• バンデタニブ vandetanib
• バタラニブ vatalanib

　 　

「上皮成長因子受容体阻害薬」

　　[★]

英

epidermal growth factor receptor inhibitor

関

上皮成長因子受容体

薬理学

• EGF受容体拮抗薬

• gefitinib, エルロチニブ erlotinib
• セツキシマブ cetuximab,トラスツズマブ trastuzumab

• BCR-ALB/C-KIT/PDGFR阻害薬

• imatinib
• dasatinib, nilotinib

• FLT3阻害薬

• PKC412(midostaurin)

• JAK2阻害薬
• RAS/MAPキナーゼ経路阻害

• tipifarnib
• lonafarnib
• sorafenib

• mTOR阻害薬

• rapamycin(sirolimus)
• temsirolimus(CCI-779)
• everolimus(RAD001)