产品说明书

Rifabutin

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Chemical Structure| 72559-06-9 同义名 : 利福布丁 ;Ansamycin;LM-427;Rifabutina;Mycobutin
CAS号 : 72559-06-9
货号 : A878035
分子式 : C46H62N4O11
纯度 : 96%
分子量 : 847.005
MDL号 : MFCD00866816
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(59.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Rifabutin (RBT) is the rifamycin that is recommended to treat tuberculosis (TB) in HIV-infected individuals during combination antiretroviral therapy (ART) containing HIV protease inhibitors (PIs)[3]. Rifabutin is a rifamycin with activity against Mycobacterium tuberculosis. RFB is well tolerated by patients who develop RMP-related (Rifampin) AEs (adverse effects)[4]. Rifabutin at 16 μg/mL was only bacteriostatic (MIC of 4 μg/mL) and was moderately synergistic in combination with imipenem (fractional inhibitory concentration [FIC] index of 0.38). Addition of rifabutin (16 μg/mL) moderately increased killing by a low (8 μg/mL) but not by a high (32 μg/mL) concentration of imipenem. In infected macrophages, rifabutin (16 μg/mL) increased the activity of imipenem at 8 and 32 μg/mL, achieving 3- and 100-fold reductions in the numbers of intracellular bacteria, respectively[5]. The use of rifabutin can improve treatment outcomes in patients with rifabutin-sensitive MDR-TB[6]. In addition, the combination of rifabutin plus bedaquiline produces sustained intracellular mycobactericidal activity that is greater than the sum of their individual effects[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02024555 Sarcoidosis; Antimycobacterial... 展开 >> Therapy 收起 << Phase 2 Recruiting May 2019 United States, New York ... 展开 >> Albany Medical Center Recruiting Albany, New York, United States, 12208 Contact: Marc Judson, MD    518-262-5196    judsonm@mail.amc.edu    Contact: Leahruth Saavedra, MS    (518) 262-0355    saavedl@amc.edu    Sub-Investigator: Marc Judson, MD          United States, Ohio University of Cincinnati Recruiting Cincinnati, Ohio, United States, 45267 Contact: Robert Baughman, MD    513-584-5110    bob.baughman@ucmail.uc.edu    Contact: Joyce Zeigler    (513) 584-6252    zeiglejm@ucmail.uc.edu    Principal Investigator: Robert Baughman, MD          Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Contact: Dan Culver, DO    216-444-6508    culverd@ccf.org    Contact: Allison Wimer    216-444-9975    wimera@ccf.org    Principal Investigator: Dan Culver, DO          Ohio State University Recruiting Columbus, Ohio, United States, 43221 Contact: Elliott Crouser, M.D.    614-293-4925    elliott.crouser@osumc.edu    Contact: Karen Martin    614-293-4978    karen.martin@osumc.edu    Sub-Investigator: Elliott Crouser, M.D.          United States, South Carolina Medical University of South Carolina Recruiting Charleston, South Carolina, United States, 29425 Contact: Ennis James, MD    843-792-3769    jamesw@musc.edu    Contact: Robyn Do    (843) 792-1221    dorobyn@musc.edu    Sub-Investigator: Ennis James, MD          United States, Tennessee Vanderbilt University School of Medicine Recruiting Nashville, Tennessee, United States, 37232 Contact: Wonder Drake, MD    615-322-2035    wonder.drake@vanderbilt.edu    Contact: Amy Kerrigan, MSN    615-343-3238    amy.kerrigan@vanderbilt.edu    Principal Investigator: Wonder Drake, MD 收起 <<
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
NCT01951326 Crohn's Disease Phase 3 Active, not recruiting April 2019 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.18mL

0.24mL

0.12mL

5.90mL

1.18mL

0.59mL

11.81mL

2.36mL

1.18mL
参考文献

[1]Katoh M, Watanabe M, et al. In vivo induction of human cytochrome P450 3A4 by rifabutin in chimeric mice with humanized liver. Xenobiotica. 2005 Sep;35(9):863-75.

[2]Kunin CM. Antimicrobial activity of rifabutin. Clin Infect Dis. 1996 Apr;22 Suppl 1:S3-13; discussion S13-4.

[3]Ramachandran G, Hemanth Kumar AK, Kannan T, et al. Pharmacokinetics of rifabutin during atazanavir/ritonavir co-administration in HIV-infected TB patients. Indian J Tuberc. 2019;66(1):129–133

[4]Horne DJ, Spitters C, Narita M. Experience with rifabutin replacing rifampin in the treatment of tuberculosis. Int J Tuberc Lung Dis. 2011;15(11):1485–i

[5]Le Run E, Arthur M, Mainardi JL. In Vitro and Intracellular Activity of Imipenem Combined with Rifabutin and Avibactam against Mycobacterium abscessus. Antimicrob Agents Chemother. 2018;62(8):e00623-18.

[6]Lee H, Ahn S, Hwang NY, et al. Treatment outcomes of rifabutin-containing regimens for rifabutin-sensitive multidrug-resistant pulmonary tuberculosis. Int J Infect Dis. 2017;65:135–141

[7]Wallis RS, Good CE, O'Riordan MA, et al. Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial. PLoS One. 2018;13(5):e0196756. Published 2018 May 2