唑喹達

唑喹達
臨床資料
其他名稱	LY-335979
ATC碼	未分配;
法律規範狀態
法律規範	研究性藥物;
識別資訊
	IUPAC命名法 (2R)-14-[(1aR,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c] [7]annulen-6-yl3-(quinolin-5-yloxy)propan-2-ol; ;
CAS號	167354-41-8
PubChem CID	153997;
DrugBank	DB06191 ;
ChemSpider	24599682 ;
UNII	AB5K82X98Y;
KEGG	D06387 ;
ChEMBL	ChEMBL444172 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID9057894 ;
ECHA InfoCard	100.236.552
化學資訊
化學式	C32H31F2N3O2
摩爾質量	527.62 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES Cl.Cl.Cl.FC4(F)[C@@H]3c1ccccc1C(c2c(cccc2)[C@@H]34)N5CCN(CC5)C[C@@H](O)COc7c6cccnc6ccc7;
	InChI InChI=1S/C32H31F2N3O2/c33-32(34)29-22-7-1-3-9-24(22)31(25-10-4-2-8-23(25)30(29)32)37-17-15-36(16-18-37)19-21(38)20-39-28-13-5-12-27-26(28)11-6-14-35-27/h1-14,21,29-31,38H,15-20H2/t21-,29-,30+,31-/m1/s1 ; Key:IHOVFYSQUDPMCN-DBEBIPAYSA-N ;

唑喹達（英語：Zosuquidar，開發代號：LY-335979），也譯作佐舒喹達，是一種實驗性抗腫瘤藥物。^[1]唑喹達可以抑制P-糖蛋白。^[2]具有這種機制的其他藥物包括他立喹達和拉尼喹達。P-糖蛋白是一種跨膜蛋白，它依賴三磷酸腺苷將異物泵出細胞。過度表達P-糖蛋白的癌症能夠在治療分子到達目標之前泵出治療分子，從而有效地使癌症具有多重耐藥性。唑喹達抑制P-糖蛋白，抑制外排泵並恢復對化療藥物的敏感性。^[2]

唑喹達最初由Syntex Corporation研發，該公司於1990年被羅氏收購。羅氏於 1997 年將該藥物許可給禮來公司。2006年被FDA授予用於急性骨髓性白血病的孤兒藥地位。2010年，該藥物被宣佈在一項治療急性骨髓性白血病和骨髓增生異常綜合症的III期臨床試驗未達到其主要終點，^[3]禮來公司並停止了對其的開發。^[4]

參考資料

^ Zosuquidar trihydrochloride. NCI Drug Dictionary. National Cancer Institute. [2023-02-20]. （原始內容存檔於2023-02-10）.
^ ^2.0 ^2.1 Cripe LD, Uno H, Paietta EM, Litzow MR, Ketterling RP, Bennett JM, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. November 2010, 116 (20): 4077–4085. PMC 2993615 . PMID 20716770. doi:10.1182/blood-2010-04-277269.
^ Clinical trial number NCT00046930 for "Daunorubicin & Cytarabine +/- Zosuquidar inTreating Older Patients With Newly Diagnosed Acute Myeloid Leukemia or Refractory Anemia" at ClinicalTrials.gov
^ Zosuquidar - Kanisa Pharmaceuticals. Adis Insight. Springer Nature Switzerland AG. [2023-02-20]. （原始內容存檔於2023-02-10）.

[1] Zosuquidar trihydrochloride. NCI Drug Dictionary. National Cancer Institute. [2023-02-20]. （原始內容存檔於2023-02-10）.

[Cripe-2] 2.0 ^2.1 Cripe LD, Uno H, Paietta EM, Litzow MR, Ketterling RP, Bennett JM, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. November 2010, 116 (20): 4077–4085. PMC 2993615 . PMID 20716770. doi:10.1182/blood-2010-04-277269.

[3] Clinical trial number NCT00046930 for "Daunorubicin & Cytarabine +/- Zosuquidar inTreating Older Patients With Newly Diagnosed Acute Myeloid Leukemia or Refractory Anemia" at ClinicalTrials.gov

[4] Zosuquidar - Kanisa Pharmaceuticals. Adis Insight. Springer Nature Switzerland AG. [2023-02-20]. （原始內容存檔於2023-02-10）.

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