SALARIUS PHARMACEUTICALS, INC. Seclidemstat (SP-2577) is a novel, oral, reversible inhibitor of lysine-specific histone demethylase 1, also referred to as LSD1, an enzyme that plays a key role in the development and progression of several cancers. Therapies designed to inhibit LSD1’s cancer-promoting activity represent a growing field of research.
Salarius believes seclidemstat uses a unique approach compared to other LSD1 inhibitors now in development by simultaneously targeting the enzymatic activity of LSD1 and its scaffolding properties, creating a dual mechanism of action that could provide differential therapeutic activity in several cancer types, including solid tumors. To date, the therapeutic activity of LSD1 inhibitors in clinical development has largely been confined to hematological cancers and myeloproliferative neoplasms.
“We are excited to be working with Salarius to further explore the potential of seclidemstat and LSD1 inhibition in new indications. Overexpression of the LSD1 enzyme is associated with poor prognosis across a variety of cancer types. Building on our prior research expertise and knowledge, we will explore the impact of LSD1 depletion and LSD1 catalytic inhibition on the transcriptome in order to better understand the enzyme’s catalytic and non-catalytic functions and the impact of seclidemstat on those functions,” Whetstine said.
“Seclidemstat’s ability to target the scaffolding property of the LSD1 enzyme has high relevance in several cancer types and could lead to potent inhibition with advantageous therapeutic properties. Insights into these aspects of LSD1 regulation could significantly impact our understanding about LSD1 function and therapeutic intervention,” added Whetstine, who has consulted for Salarius and served the company in an advisory capacity.
A Phase 1/2 clinical trial is now underway exploring seclidemstat as a therapy for sarcomas. This trial is treating patients with myxoid liposarcoma and other FET-rearranged sarcomas with single-agent seclidemstat and evaluating seclidemstat in combination with the chemotherapy agents topotecan and cyclophosphamide as a potential second- and third-line therapy for Ewing sarcoma, a deadly pediatric bone cancer.
Recently, Salarius’ clinical program for seclidemstat expanded into hematologic cancers, with the
“This is an exciting opportunity to advance our development of seclidemstat by harnessing the scientific expertise of a renowned cancer research center and one of the rising stars in the field of LSD1 inhibition,” stated
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