Drug intelligence / Profile preview

valproic acid + dexamethasone

Development stage
Unknown
Lead developer
Barbara Ann Karmanos Cancer Institute
Modality
Small Molecules
Administration
Oral
01

Overview

Valproic acid + dexamethasone is a combination regimen investigated by the Barbara Ann Karmanos Cancer Institute in a Phase 1 pilot study (NCT02520115). This combination utilizes the synthetic corticosteroid dexamethasone and the histone deacetylase (HDAC) inhibitor valproic acid to induce the expression of folate receptor alpha (FRα) in patients with adnexal masses or ovarian carcinoma. The primary objective of this induction is to elevate serum FRα levels to serve as a diagnostic and surveillance biomarker, potentially improving the differentiation between benign and malignant masses and monitoring for cancer recurrence. Dexamethasone acts as a glucocorticoid receptor agonist, while valproic acid provides epigenetic modulation via HDAC inhibition to facilitate the induction of the biomarker.

Other names
dexamethasonevalproic acidVPAdexamethasone-Barbara Ann Karmanos Cancer Institute-ovarian carcinoma-adnexal mass
02

Targets

GR (Glucocorticoid receptor)CTNNB1 (Beta-catenin)Kir (Inward-rectifier potassium channels)CYP3A4 (Cytochrome P450 3A4)HDAC (HDAC family)

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