DDInter1762 DDInter1435
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
Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor. Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.[A182240,L7901] Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients. While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence. Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT. Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.
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