Drug intelligence / Profile preview

conolidine

Development stage
Preclinical
Lead developer
Biomia
Modality
Small Molecules
Administration
Oral, Inhalation, Intranasal, Parenteral, Subcutaneous, Intravenous, Intramuscular, Intraperitoneal, Transdermal, Topical, Rectal, Vaginal, Sublingual
01

Overview

Conolidine is a naturally occurring indole alkaloid, originally isolated from the bark of *Tabernaemontana divaricata*, that is being developed as a novel non-opioid analgesic. Unlike traditional opioids that directly activate mu-opioid receptors, conolidine acts as a potent antagonist of the atypical chemokine receptor 3 (ACKR3), also known as CXCR7. ACKR3 functions as a scavenger receptor that binds and degrades endogenous opioid peptides such as enkephalins and dynorphins. By inhibiting ACKR3, conolidine increases the local concentration of these endogenous opioids, thereby enhancing natural pain-suppression pathways. Biomia is currently advancing synthetic analogs of conolidine, including BMC-007, BMC-009, and BMC-014, for the treatment of post-surgical and chronic pain, aiming to provide effective analgesia without the side effects of addiction or respiratory depression associated with conventional opioid therapies.

Other names
conolidine
02

Targets

ACKR3 (Atypical chemokine receptor 3 (ACKR3) mRNA)CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)

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