Cimaher

Cimaher Mechanism of Action

nimotuzumab

Manufacturer:

Innogene Kalbiotech

Distributor:

Maxxcare

Marketer:

Mega Lifesciences
Full Prescribing Info
Action
Pharmacology: Nimotuzumab binds with intermediate affinity and high specificity to the extracellular domain of epidermal growth factor receptor (EGFR, HER1, c-Erb-1). Nimotuzumab blocks the binding of the EGF and other ligands such as transforming growth factor-alpha, etc, to its receptor and inhibits in vivo and in vitro tumor cell growth. Nimotuzumab has a potent anti-angiogenic, anti proliferative and pro-apoptotic effects, and also decrease motility, cell invasion and metastasis in those tumors that overexpress the EGFR.
EGFR is expressed in cells from all three embryonic layer cells especially in cells of epithelial origin (skin, respiratory tract, gastrointestinal tract, urinary tract and liver). EGFR is present in wide diversity of human tumors of epithelial origin like non small cell lung cancer (NSCLC), head and neck, pancreatic, colon, breast, kidney, ovarian and bladder carcinomas. It is also overexpressed in glioma and uterine cervical cancers.
Pharmacokinetics: Nimotuzumab administered in combination with concomitant chemotherapy or radiotherapy exhibits nonlinear pharmacokinetics. Following a 30 minute infusion the area under the concentration time curve (AUC) increased in a greater than dose proportional manner as the dose increased from 50 to 400 mg. Evidence from an animal pharmacokinetic study indicates that the concentration of the antibody in tumors is highest at 24 hours after injection. In humans, the volume of the central compartment (Vc) for Nimotuzumab ranged from 2.3 to 7.2 L and maximal concentration (Cmax) was 27 to 57 ng/mL for 50 to 400 mg doses, respectively. Nimotuzumab is mainly distributed in liver, spleen, heart, kidney and bladder. Most of the antibodies were uptake by liver.
Nimotuzumab clearance (CL) decreased from 1.08-0.34 mL/h/kg as the dose increased from 50 to 200 mg, and at doses >200 mg, it appeared to plateau. Pharmacokinetic analysis of plasma clearance curves showed terminal half-life times (t½b) for 50, 100, 200 and 400 mg doses of 62, 82, 302 and 304 hours, respectively. Under normal physiological conditions, the percentage of injected dosage discharged through urinary tract are 21.1% for 50 mg, 28.20% for 100 mg, 27.36% for 200 mg, 33.57% for 400 mg.
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