Nimotuzumab
L01XC | |
|---|---|
| Pharmacokinetic data | |
| Elimination half-life | 62–304 hours |
| Identifiers | |
| CAS Number | |
| ChemSpider |
|
| UNII | |
| Chemical and physical data | |
| Formula | C6566H10082N1746O2056S40[1] |
| Molar mass | 147659.45 g·mol−1 |
  (what is this?) (verify) | |
Nimotuzumab (h-R3,
Like cetuximab, nimotuzumab binds to the epidermal growth factor receptor (EGFR), a signalling protein that normally controls cell division. In some cancers, this receptor is altered to cause uncontrolled cell division, a hallmark of cancer. These monoclonal antibodies block EGFR and stop the uncontrolled cell division.
It has a humanized human-mouse h-R3 heavy chain and a humanized human-mouse h-R3 κ-chain.[1][4]
Mechanism
Nimotuzumab binds with optimal affinity and high specificity to the extracellular region of EGFR (epidermal growth factor receptor). This results in a blockade of ligand binding and receptor activation. Epidermal growth factor receptor (EGFR) is a key target in the development of cancer therapeutics. EGFR-targeting drugs have been shown to improve response when used with conventional treatments such as radiation therapy and chemotherapy.[2]
Development status
It was developed at the
CIMYM BioSciences licensed European rights to nimotuzumab to Oncoscience AG in 2003, the South Korean rights to Kuhnil Pharmaceutical Co., Ltd. in 2005, and in 2006, licensed the Japanese rights to Daiichi Sankyo and rights to certain countries in Asia and Africa to Innogene Kalbiotech Pte Ltd.[6] Other licensees for nimotuzumab include Biocon BioPharmaceuticals Ltd. (BBPL) in India, Biotech Pharmaceutical Co. Ltd. in China, Delta Laboratories in Colombia, European Chemicals SAC, Quality Pharma in Peru, Eurofarma Laboratorios Ltda. in Brazil, Ferozsons Labs in Pakistan, Laboratorio Elea S.A.C.I.F.yA. in Argentina, EL KENDI Pharmaceutical in Algeria and Laboratorios PiSA in Mexico.[citation needed]
In December 2012, CIMYM BioSciences dissolved and sold its assets related to nimotuzumab to InnoKeys PTE Ltd.[7]
According to a 2009 review: "Nimotuzumab was approved for the following indications—For
As of 2014 Nimotuzumab was in additional Phase I and II clinical trials.[8]
In April 2014, Daiichi Sankyo announced that it was halting a multicenter, randomized, double-blind, placebo-controlled Phase III study investigating nimotuzumab for first-line therapy in patients with unresectable and locally advanced
Safety
The toxicity and safety of nimotuzumab have been assessed in several pre-clinical and clinical studies wherein it was noticed that side effects usually caused by EGFR inhibitors, especially rashes and other skin toxicities, were negligible. Scientists have hypothesized that this is because nimotuzumab binds only to cells that express moderate to high EGFR levels.[2]
Nimotuzumab has been found to be very well tolerated in clinical trials. Common adverse reactions seen in patients treated with nimotuzumab include:[10][11]
- Chills
- Fever
- Nausea and vomiting
- Dryness of mouth
- Asthenia
- Hypertension/hypotension
- Flushing
Notes
- ^ a b WHO Drug Information, Vol. 19, No. 4, 2005 Proposed INN List 94, p.333
- ^ PMID 20046573.
- ^ BIOMAb EGFR (Biocon, India)
- ^ Merck Index 14th Edition Monograph number 10585.
- PMID 9154469.
- ^ a b YM Biosciences YM Biosciences Annual Report for year ended June 30, 2007 Archived September 7, 2017, at the Wayback Machine
- ^ YM Biosciences press release. December 2012 YM BioSciences Reports Divestiture of Nimotuzumab Assets by CIMYM
- PMID 24605265.
- ^ Daiichi Sankyo press release. April 25, 2014 Daiichi Sankyo Announces Discontinuation of Phase 3 Clinical Trial in Japan of Nimotuzumab (DE-766) in Lung Cancer
- ^ TheraCIM Official Site
- ^ BioMab Insert