Drug intelligence / Profile preview

DLBS1442

Development stage
Phase 2
Lead developer
Dexa Medica
Modality
Small Molecules
Administration
Oral
01

Overview

DLBS1442 is a proprietary, standardized semipolar bioactive fraction extracted from the fruit of the Indonesian plant Phaleria macrocarpa (Scheff.) Boerl (family Thymelaceae). It is developed as an oral small molecule therapy primarily for gynecological conditions such as endometriosis, primary dysmenorrhea, and premenstrual syndrome. Mechanistically, DLBS1442 exhibits antiangiogenic, anti-inflammatory, and proapoptotic activities. In vitro studies show that it inhibits angiogenesis by downregulating vascular endothelial growth factor (VEGF), hypoxia-inducible factor 1-alpha (HIF-1α), and matrix metalloproteinases MMP-9 and MMP-2; reduces nuclear factor kappa B (NFκB) activity; downregulates estrogen receptor expression while upregulating progesterone receptor expression; suppresses the eicosanoid pathway; induces apoptosis in endometrial cells via caspase-8 activation; and decreases cell viability in a dose-dependent manner[5][10][7]. Clinical studies indicate efficacy in reducing pain associated with endometriosis and dysmenorrhea as well as alleviating symptoms of premenstrual syndrome[1][9]. The drug has been evaluated up to Phase 3 clinical trials for endometriosis but is not yet approved in any country[2].

Brand names
DLBS1442DLBS-1442DLBS 1442
Other names
Phaleria macrocarpa bioactive fraction
02

Targets

ER (Estrogen receptor)VEGFA (Vascular endothelial growth factor A)NFKB1 (NF-κB1)MMP9 (Matrix metalloproteinase-9)HIF1A (Hypoxia-inducible factor 1-alpha)PR (Progesterone receptor)

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