Delving into the Latest Updates on Methylcantharidimide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Methyl cantharidimide, 甲基斑蝥二胺片, 甲基斑蝥胺

Target-

Mechanism-

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Liver Cancer

Inactive Indication-

Originator Organization

Jiangsu Sihuan Bioengineering Co., Ltd.

Active Organization

Jiangsu Sihuan Bioengineering Co., Ltd.

Tonghua Wantong Pharmaceutical Co. Ltd.

Chongqing Pharmaceutical Research Institute Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (01 Jan 1990),

Liver Cancer

Regulation-

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Structure

Molecular FormulaC11H15NO3

InChIKeyWUQNOBSCYAIJIH-FIPCFZRWSA-N

CAS Registry76970-78-0

Beagle dogs were randomly divided into negative control group(blank tablet), methyl cantharidimide tablets group (6.11,12.21, 24.42 mg x kg(-1)), continuously 30 days of oral adminiStration, once a day. The drug and control group were collected and determined fresh urine in 1, 2, 3 and 4 weeks of the administration; Serum urea nitrogen (BUN), creatinine (Crea), total protein (TP) and albumin (ALB) as well as sodium, potassium, chloride electrolyte were determined on 15 and 30 days of the administration; Urine albumin (mAlb), kidney injury molecule-1 (KIM-1), neutrophil gelatinase-associated lipocalin( NGAL), N-acetyl-beta-D-glucosaminidase (NAG), clusterin, beta2-microglobulin (beta2-MG), alpha1-microglobulin (alpha1-MG), alanine aminopeptidase( AAP) and im- munoglobulins IgG were tested on 15 and 30 days of the administration.

RESULT:

Compared with the control group, urine protein and white blood cells was significantly increased in each dose group. On 15 days of the administration, mAlb were higher in each dose group, KIM-1, NGAL, clusterin, NAG and AAP were significantly higher in high-dose group, while the middle and low dose group had no significant difference, as well as blood SCr and BUN no obvious abnormalities. On 30 days, mAlb, KIM-1, clusterin, NAG, AAP were increased in each dose group, appearing dose-effect relationship, beta2-MG and NGAL levels were significantly increased in high-dose group. Contents above indicators were increased with significant dose and time relationship, and serum BUN, Scr were correlated, suggesting that urine mAlb, KIM-1, clusterin, NAG and AAP indicators that can sensitively respond the changes of proteins and enzymes in urine.

CONCLUSION:

Methyl cantharidimide tablets has a renal toxicity, urine mAlb, KIM-1, clusterin, NAG and AAP can be used as the early nephrotoxic biomarkers of methyl cantharidimide tablets.

01 Nov 2013·Chemical biology & drug designQ4 · MEDICINE

Cantharidin‐Based Small Molecules as Potential Therapeutic Agents

Q4 · MEDICINE

Review

Author: Vargas Méndez, Leonor Y. ; Puerto Galvis, Carlos E. ; Kouznetsov, Vladimir V.

Chemical and pharmacological information on cantharidin‐based small molecules was analyzed. The review summarizes new facts about blister beetles' metabolites for the period 2006–2012. General synthetic approaches to cantharidin‐based small molecules as well as their chemical transformations and biological activities related to cantharidin, norcantharidin, cantharidimide, and norcantharimide analogs, especially their inhibitory activity of phosphoprotein phosphatases in cancer treatment, were discussed in this mini review, which could help to design new small molecule modulators for other biological models.

01 Oct 2010·Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica

Determination of plasma concentration of N-methylcantharidimide by HPLC and its pharmacokinetics after intravenous administration in dogs

Article

Author: Xiaobo Wu ; Xianqin Luo

OBJECTIVES:

To establish a HPLC method for determination of N-methylcantharidimide in dogs' plasma and to study the pharmacokinetics of N-methylcantharidimide in dogs'.

METHOD:

The plasma samples were extracted by methanol. The acetonitrile and the purified water composed mobile phase. The flow rate was 0. 7 mL x min(-1), ultraviolet detection wavelength was at 212 nm.

RESULT:

The calibration curve was linear over the range from 0.01-10.0 mg x L(-1) with a correlation coefficiency of 0.996 3. The lower limit of quantitation was 0.01 mg x L(-1). The mean recovery was 92.3%. the relative standard deviation (RSD) of intra-day and inter-day were all less than 10%. After intravenous administration of N-methylcantharidimide with 3 dosages of 10, 15, 20 mg x kg(-1) to dogs, the corresponding distribution half-livers (t1/2alpha) were 1.8, 2.1, 1.7 min, and the elimination half-lives (t1/2beta) were 144,139, 146 min, respectively.

CONCLUSION:

This method is convenient, accurate and reliable. It can be used for determination of N-methylcantharidimide in dogs' plasma and pharmacokinetic studies.

100 Deals associated with Methylcantharidimide

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