Temozolomide Pellets

(Product under development)
Temozolomide PelletsTemozolomide (brand names Temodar and Temodal is an oral alkylating agent which can be used for the treatment of Grade IV astrocytoma — an aggressive brain tumor, also known as glioblastoma multiforme as well as melanoma, a form of skin cancer.

It is also indicated for Grade III Anaplastic Astrocytoma and not indicated for, but now used to treat oligodendroglioma brain tumors in some countries, replacing the older (and less well-tolerated) PCV (Procarbazine-Lomustine-Vincristine) regimen.

The agent was developed by Malcolm Stevens and his team at Aston University in Birmingham, A derivative of imidazotetrazine, temozolomide is the prodrug of MTIC (3-methyl-(triazen-1-yl)imidazole-4-carboxamide). It has been available in the US since August 1999, and in other countries since the early 2000s.

The therapeutic benefit of temozolomide depends on its ability to alkylate/methylate DNA, which most often occurs at the N-7 or O-6 positions of guanine residues. This methylation damages the DNA and triggers the death of tumor cells.

However, some tumor cells are able to repair this type of DNA damage, and therefore diminish the therapeutic efficacy of temozolomide, by expressing an enzyme called O-6-methylguanine-DNA methyltransferase (MGMT) or O-6-alkylguanine-DNA alkyltransferase (AGT or AGAT).

In some tumors, epigenetic silencing of the MGMT/AGT gene prevents the synthesis of this enzyme, and as a consequence such tumors are more sensitive to killing by temozolomide. Conversely, the presence of MGMT protein in brain tumors predicts poor response to temozolomide and these patients receive little benefit from chemotherapy with temozolomide.

Available Form:
Temozolomide Pellets
Temozolomide Granules

Umang Pharmatech equipments used for production of Temozolomide Pellets:
Drug Layering, Fluid Bed Dryer, Fluid Bed Coater, Sifter & Blender, Extruder and Twin spheronizer.

Temozolomide Pellets
Systematic (IUPAC) Name
Temozolomide Pellets
Identifiers
Temozolomide Pellets
Chemical data
4-methyl-5-oxo- 2,3,4,6,8-pentazabicyclo [4.3.0] nona-2,7,9-triene- 9-carboxamide
CAS number : 85622-93-1
ATC code : L01AX03
PubChem : CID 5394
DrugBank : APRD00557
ChemSpider : 5201
UNII : YF1K15M17Y
KEGG : D06067
ChEMBL : CHEMBL810
Formula : C6H6N6O2
Mol. mass : 194.151 g/mol


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