阿拉韦罗
阿拉韦罗(INN:Aplaviroc;开发代号:AK602和GSK-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。
臨床資料 | |
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给药途径 | Oral |
ATC碼 |
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法律規範狀態 | |
法律規範 |
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识别 | |
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CAS号 | 461443-59-4 461023-63-2 |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII |
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KEGG | |
ChEMBL | |
CompTox Dashboard (EPA) | |
化学 | |
化学式 | C33H43N3O6 |
摩尔质量 | 577.72 g·mol−1 |
3D模型(JSmol) | |
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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
- Borthwick AD. . Chemical Reviews. July 2012, 112 (7): 3641–3716. PMID 22575049. doi:10.1021/cr200398y.
- 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).
- 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 . PMID 15681411. doi:10.1128/jvi.79.4.2087-2096.2005.
- . AIDSmeds.com. October 25, 2005 [September 5, 2008]. (原始内容存档于January 13, 2007).
- 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 . PMID 18070967. doi:10.1128/aac.00821-07.
- Moyle G. . The Body. December 19, 2006 [September 5, 2008]. (原始内容存档于6 October 2008).
- 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 .
延伸阅读
- Horster S, Goebel FD. . Infection. April 2006, 34 (2): 110–113. PMID 16703305. S2CID 38463200. doi:10.1007/s15010-006-6206-1.
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