Drug intelligence / Profile preview

ENGA-L06E

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

ENGA-L06E is a novel **aza-steroidal alkylating ester** synthesized as an anticancer agent specifically investigated for activity against human ovarian carcinoma. Mechanistically, it acts as a **dual inhibitor** of the **PI3K-AKT** and **KRAS-ERK** signaling pathways, which are critically involved in the survival and proliferation of ovarian cancer cells. ENGA-L06E is structurally distinct from classic non-steroidal alkylators (such as POPAM and melphalan) and has demonstrated significantly higher **cytostatic and cytotoxic activity** both in vitro and in vivo models, with a lower toxicity profile. The compound's efficacy is independent of mutations in TP53, KRAS, MEK1, or PIK3CA, as well as mismatch repair or steroid receptor status. It has also shown promising effects in overcoming resistance to alkylating agents, partly due to its reported ability to inhibit PARP activity. These properties indicate its potential as a next-generation therapy for chemoresistant epithelial ovarian carcinoma[1].

02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)AKT (RAC-alpha serine/threonine-protein kinase)MAPK3 (Mitogen-activated protein kinase 1)DNA

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