Delving into the Latest Updates on SCO-201 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

ABCA1

Mechanism

ABCA1 stimulants(ATP binding cassette subfamily A member 1 stimulants)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Solid tumor

Originator Organization

Scandion Oncology A/S

Active Organization-

Inactive Organization

Scandion Oncology A/S

Drug Highest PhaseSuspendedPreclinical

First Approval Date-

Regulation-

ATP-binding cassette (ABC) transporters, such as breast cancer resistance protein (BCRP), are key players in resistance to multiple anti-cancer drugs, leading to cancer treatment failure and cancer-related death. Currently, there are no clinically approved drugs for reversal of cancer drug resistance caused by ABC transporters. This study investigated if a novel drug candidate, SCO-201, could inhibit BCRP and reverse BCRP-mediated drug resistance. We applied in vitro cell viability assays in SN-38 (7-Ethyl-10-hydroxycamptothecin)-resistant colon cancer cells and in non-cancer cells with ectopic expression of BCRP. SCO-201 reversed resistance to SN-38 (active metabolite of irinotecan) in both model systems. Dye efflux assays, bidirectional transport assays, and ATPase assays demonstrated that SCO-201 inhibits BCRP. In silico interaction analyses supported the ATPase assay data and suggest that SCO-201 competes with SN-38 for the BCRP drug-binding site. To analyze for inhibition of other transporters or cytochrome P450 (CYP) enzymes, we performed enzyme and transporter assays by in vitro drug metabolism and pharmacokinetics studies, which demonstrated that SCO-201 selectively inhibited BCRP and neither inhibited nor induced CYPs. We conclude that SCO-201 is a specific, potent, and potentially non-toxic drug candidate for the reversal of BCRP-mediated resistance in cancer cells.

100 Deals associated with SCO-201

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