DDInter1642 DDInter1762
Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein.
Refractory anaplastic astrocytoma (WHO grade III) and Glioblastoma multiforme (WHO grade IV) are primary malignant brain tumours with poor prognosis and limited treatment options. Despite considerable genetic heterogeneity, these tumours often have impaired DNA repair systems, rendering them initially sensitive to alkylating agents, although they invariably develop resistance to these agents over time.[A229848, A229858, L32033] Temozolomide is an imidazotetrazine prodrug that is stable at acidic pH but undergoes spontaneous nonenzymatic hydrolysis at neutral or slightly basic pH; these properties allow for both oral and intravenous administration.[A229853, A229888, A229923, L32033] Following initial hydrolysis, further reactions liberate a highly reactive methyl diazonium cation capable of methylating various residues on adenosine and guanine bases leading to DNA lesions and eventual apoptosis.[A229853, A229923] Temozomolide as an adjunct to radiotherapy followed by maintenance dosing remains the standard of care for both Glioblastoma and refractory anaplastic astrocytoma. Temozolomide was granted FDA approval on August 11, 1999, as an oral capsule and subsequently on February 27, 2009, as an intravenous injection. It is currently marketed under the trademark TEMODAR® by Merck.
Temozolomide {u} (Compound) treats {v} (Disease) brain cancer
Temozolomide {u} (Compound) binds {v} (Gene) CYP3A4
Temozolomide {u} (Compound) upregulates {v} (Gene) CAPN1
Temozolomide {u} (Compound) is included by {v} (Pharmacologic Class) Alkylating Activity
Temozolomide {u} (Compound) downregulates {v} (Gene) ATP6V1D
Temozolomide {u} (Compound) causes {v} (Side Effect) Constipation
Temozolomide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sparfloxacin
Temozolomide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Enoxacin
Temozolomide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Fluorouracil
Temozolomide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Naxitamab
Temozolomide (Compound) treats brain cancer (Disease)
Temozolomide (Compound) binds CYP3A4 (Gene)
Temozolomide (Compound) upregulates CAPN1 (Gene)
Temozolomide (Compound) is included by Alkylating Activity (Pharmacologic Class)
Temozolomide (Compound) downregulates ATP6V1D (Gene)
Temozolomide (Compound) causes Constipation (Side Effect)
Temozolomide may cause a minor interaction that can limit clinical effects when taken with Sparfloxacin
Temozolomide may cause a minor interaction that can limit clinical effects when taken with Enoxacin
Temozolomide may cause a moderate interaction that could exacerbate diseases when taken with Fluorouracil
Temozolomide may cause a moderate interaction that could exacerbate diseases when taken with Naxitamab