异烟肼/胡椒碱/利福平(Isoniazid/Piperine/Rifampicin) - 药物靶点：CYP3A x P-gp x RNAP_在研适应症：结核，肺结核_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Risorine

靶点

CYP3A x P-gp x RNAP

作用机制

CYP3A抑制剂(细胞色素P450家族成员3A家族抑制剂)、P-gp抑制剂(P-糖蛋白-1抑制剂)、RNAP抑制剂(细菌DNA指导的RNA聚合酶复合体抑制剂)

治疗领域

感染呼吸系统疾病

在研适应症

结核肺结核

非在研适应症-

原研机构

Cadila Pharmaceuticals Ltd.

在研机构

Cadila Pharmaceuticals Ltd.

Zydus Lifesciences Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

印度 (2009-10-16),

结核

最高研发阶段(中国)-

特殊审评-

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结构

分子式C43H58N4O12

InChIKeyJQXXHWHPUNPDRT-ZNQWNCHJSA-N

CAS号13292-46-1

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关联

4

项与异烟肼/胡椒碱/利福平相关的临床试验

CTRI/2017/04/008329 / Not yet recruiting临床4期IIT

An open label, Balanced, Randomized, Active control clinical trial to compare Safety and Efficacy of Risorine Capsule in adult patients with RNTCP Category I Pulmonary Tuberculosis

开始日期2017-04-17

申办/合作机构-

CTRI/2012/11/003096 / Completed临床4期

TO STUDY EFFECT OF RISORINE THERAPY ON PLASMA RIFAMPICIN LEVELS IN PATIENTS WHO REMAIN SPUTUM POSITIVE AT THE END OF 8 WEEKS OF CONVENTIONAL INTENSIVE PHASE THERAPY

开始日期2012-06-10

申办/合作机构

Cadila Pharmaceuticals Ltd.

CTRI/2012/06/002742 / Completed临床4期

Efficacy and Safety Study of Risorine (FDC of Rifampicin 200mg + Isoniazid 300mg + Piperine 10mg) in Patients with Newly Diagnosed Sputum Smear Positive Pulmonary Tuberculosis: a Randomized, Single-blind, Comparative Clinical Trial

开始日期2011-02-10

申办/合作机构-

100 项与异烟肼/胡椒碱/利福平相关的临床结果

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100 项与异烟肼/胡椒碱/利福平相关的转化医学

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100 项与异烟肼/胡椒碱/利福平相关的专利（医药）

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3

项与异烟肼/胡椒碱/利福平相关的文献（医药）

2017-09-01·The Journal of the Association of Physicians of India

A Randomized, Controlled, Phase III Clinical Trial to Evaluate the Efficacy and Tolerability of Risorine with Conventional Rifampicin in the Treatment of Newly Diagnosed Pulmonary Tuberculosis Patients.

Article

作者: Vora, Agam ; Jagannath, K ; Patel, Mukesh ; Patel, Anand ; Patel, Naresh

BACKGROUNDThe overall goals for treatment of Tuberculosis (TB) are to cure individual patient and to minimize the transmission of Mycobacterium tuberculosis. At the time of study conduction, the standard treatment for newly diagnosed tuberculosis patients consisted of an intensive phase for two months with four drugs (HRZE), followed by continuation phase for four months with two drugs (HR). Rifampicin, which is very effective against Mycobacterium tuberculosis, in both the phases of treatment, has certain concerns, which includes, decreased bioavailability with chronic use and hepatotoxicity. To overcome these concerns a new boosted formulation of Rifampicin (Risorine) with bio-enhancer Piperine was developed. Piperine has been found to increase bioavailability of several drugs including Amoxicillin, Cefotaxime, Theophylline and Propranolol. Risorine is a fixed dose combination that contains Rifampicin 200 mg + Isoniazid 300 mg + Piperine 10 mg.AIM AND OBJECTIVEThe aim of the present study was to validate the therapeutic efficacy and tolerability of Risorine formulation containing regimen with a conventional regimen in the management of patients with newly diagnosed pulmonary tuberculosis.METHODSTotal 216 patients with sputum positive and treatment naïve pulmonary tuberculosis were enrolled in the study after fulfillment of inclusion / exclusion criteria. These patients were randomized to receive either a conventional anti-TB therapy (n = 117) or a similar regimen containing Risorine (n = 99) for 6 months. During the study period, symptomatic improvement, sputum conversion and radiological improvement were monitored at regular intervals.RESULTSOf the 216 enrolled patients, 75% in the Risorine group and 79% in the control group completed the study. At 4 weeks the sputum conversion rate was significantly superior in Risorine group (93%) than the control group (84%), which was consistence throughout the study. Cure rate at the end of 24 weeks, was higher in Risorine group (92%) than in the control group (82%). Elevation of liver enzymes were observed in 3 patients in the Risorine group and in 9 patients in control group.CONCLUSIONSRisorine, a novel formulation of low dose Rifampicin (200 mg), a bio enhancer Piperine (10 mg) and standard dose Isoniazid (300 mg) when given along with Ethambutol and Pyrazinamide was comparable in efficacy with standard WHO therapy using conventional formulation. Risorine provides more Rifampicin in blood compare to GI tract as well as maintaining higher blood levels on chronic therapy compared to conventional Rifampicin with better safety profile. Risorine gives higher sputum conversion rate during the Intensive Phase which is maintained till the end of study. Further a trend was also noticed towards better tolerability with newer formulation, Risorine. H = Isoniazid, R = Rifampicin, Z = Pyrazinamide and E = Ethambutol.

2016-11-01·The Journal of the Association of Physicians of India

Role of Risorine in the Treatment of Drug - Susceptible Pulmonary Tuberculosis: A Pilot Study.

Article

作者: Vora, Agam ; Patel, Kamlesh ; Patel, Sanjay

OBJECTIVETo study the efficacy and tolerability of Risorine Capsule (A fixed dose combination of Rifampicin 200 mg + INH 300 mg + Piperine 10 mg) therapy in the treatment of drug-susceptible pulmonary tuberculosis patients who developed GI intolerance with standard WHO anti TB regimen.METHODS33 patients with pulmonary tuberculosis were treated with one Risorine kit, daily consisting of one capsule of Risorine, one tablet of ethambutol (800 mg) and two tablets of Pyrazinamide 750 mg each, for first two months of therapy. All the patients received one capsule of Risorine daily for next four months. Symptomatic improvement, Sputum conversion and radiological improvement were monitored at regular intervals.RESULTSOut of 27 patients who were sputum positive at baseline, 24 patients became sputum negative during the first two months of treatment. Out remaining three patients, one became sputum negative at the end of third month of treatment and the other two became sputum negative at the end of sixth month of treatment. Out of 33 patients, only two patients developed mild nausea, which subsided spontaneously. One patient who was HIV positive, developed hepatitis.CONCLUSIONSRisorine, a novel formulation of rifampicin 200 mg with bioenhancer piperine 10mg, is found to be highly effective and well tolerated in the treatment of drug - susceptible pulmonary tuberculosis.

2011-01-01·International Journal of Applied and Basic Medical Research

Bioenhancers from mother nature and their applicability in modern medicine

Article

作者: Jagdev Singh Kullar ; Rajkumar ; Gurpreet Kaur Randhawa

Concept of bioenhancers or biopotentiators was first time reported in 1929 by Bose. A bioenhancer is an agent capable of enhancing bioavailability and efficacy of a drug with which it is co-administered, without any pharmacological activity of its own at therapeutic dose used. Development and consequent isolation of these molecules, such as piperine and quercetin, is considered as scientific breakthrough. A fixed drug combination (Risorine) of rifampicin, isoniazid, and piperine is the result of this research. It contains almost 60% less dose of rifampicin because of its increased bioavailability and it also prevents resistance. This concept is mentioned as yogvahi in ayurveda and was used to increase the effect of medicines by increasing oral bioavailability, decreasing adverse effects and to circumvent parenteral routes of drug administration. More such useful and economically viable drug combinations can be developed by integrating knowledge of time tested ayurveda with modern methods of research. This review is an account of these bioenhancers, available from the natural resources.

100 项与异烟肼/胡椒碱/利福平相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	J04AC51	-

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
结核	印度	Cadila Pharmaceuticals Ltd.	2009-10-16
肺结核	-	Zydus Lifesciences Ltd.	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


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