阿拉韦罗

阿拉韦罗INN:Aplaviroc;开发代号:AK602GSK-873140)是一种 CCR5 进入抑制剂,属于2,5-二酮哌嗪类,[1]为治疗HIV感染而开发。[2][3]它是由葛兰素史克开发的。

阿拉韦罗
臨床資料
给药途径Oral
ATC碼
  • 未分配
法律規範狀態
法律規範
  • Development terminated
识别
  • 4-(4-{[(3R)-1-butyl-3-[(R)-cyclohexylhydroxymethyl]-2,5-dioxo- 1,4,9-triazaspiro[5.5]undecan-9-yl]methyl}phenoxy)benzoic acid
CAS号461443-59-4  checkY
461023-63-2  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
化学
化学式C33H43N3O6
摩尔质量577.72 g·mol−1
3D模型(JSmol
  • CCCCN1C(=O)[C@H](NC(=O)C12CCN(CC2)CC3=CC=C(C=C3)OC4=CC=C(C=C4)C(=O)O)[C@@H](C5CCCCC5)O
  • InChI=1S/C33H43N3O6/c1-2-3-19-36-30(38)28(29(37)24-7-5-4-6-8-24)34-32(41)33(36)17-20-35(21-18-33)22-23-9-13-26(14-10-23)42-27-15-11-25(12-16-27)31(39)40/h9-16,24,28-29,37H,2-8,17-22H2,1H3,(H,34,41)(H,39,40)/t28-,29-/m1/s1 checkY
  • Key:GWNOTCOIYUNTQP-FQLXRVMXSA-N checkY

2005年10月,由于肝毒性问题,所有阿拉韦罗研究均停止。[4][5]一些作者声称,疗效不佳的证据可能导致该药物的开发终止;[6]ASCENT研究是已终止的试验之一,该研究表明阿拉韦罗即使在高浓度下对许多患者也无效。[7]

参见

  • CCR5受体拮抗剂

参考资料

  1. Borthwick AD. . Chemical Reviews. July 2012, 112 (7): 3641–3716. PMID 22575049. doi:10.1021/cr200398y.
  2. Maeda K, Ogata H, Harada S, Tojo Y, Miyakawa T, Nakata H, et al. (PDF). 11th conference on retroviruses and opportunistic infections. San Francisco, CA. 2004. (原始内容 (PDF)存档于November 3, 2005).
  3. Nakata H, Maeda K, Miyakawa T, Shibayama S, Matsuo M, Takaoka Y, et al. . Journal of Virology. February 2005, 79 (4): 2087–2096. PMC 546550可免费查阅. PMID 15681411. doi:10.1128/jvi.79.4.2087-2096.2005.
  4. . AIDSmeds.com. October 25, 2005 [September 5, 2008]. (原始内容存档于January 13, 2007).
  5. Nichols WG, Steel HM, Bonny T, Adkison K, Curtis L, Millard J, et al. . Antimicrobial Agents and Chemotherapy. March 2008, 52 (3): 858–865. PMC 2258506可免费查阅. PMID 18070967. doi:10.1128/aac.00821-07.
  6. Moyle G. . The Body. December 19, 2006 [September 5, 2008]. (原始内容存档于6 October 2008).
  7. Currier J, Lazzarin A, Sloan L, Clumeck N, Slims J, McCarty D, et al. . Antiviral Therapy. 2008, 13 (2): 297–306. PMID 18505181. S2CID 21839689. doi:10.1177/135965350801300204可免费查阅.

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