Iclepertin FDA Approval Status
Last updated by Judith Stewart, BPharm on Jan 21, 2025.
FDA Approved: No
Generic name: iclepertin
Company: Boehringer Ingelheim Pharmaceuticals, Inc.
Treatment for: Cognitive Impairments Associated with Schizophrenia (CIAS)
Iclepertin is an investigational glycine transporter 1 (GlyT1) inhibitor in development for the treatment of cognitive impairments associated with schizophrenia.
- Schizophrenia is a psychiatric disorder characterised by symptoms that include delusions, hallucinations, social withdrawal, lack of motivation, and cognitive impairments. Cognitive impairments associated with schizophrenia (CIAS) include difficulties with problem solving, paying attention and memory. Currently there are no approved pharmacotherapies for the treatment of CIAS.
- A potential cause for CIAS is thought to be an imbalance in excitatory and inhibitory signalling due to NMDA receptor hypofunction.
- Iclepertin (BI 425809) is a GlyT1 inhibitor that works to normalise NMDA receptor hypofunction by blocking the reuptake of glycine to increase synaptic glycine levels, and enhance glutamatergic signalling and synaptic plasticity.
- Phase I studies have shown iclepertin to be safe and well tolerated in healthy volunteers, and central target engagement (inhibition of GlyT1) was achieved in a dose-dependent manner from 5 to 50 mg in healthy volunteers. A Phase II study has demonstrated that iclepertin is safe and well tolerated in patients with schizophrenia and improves cognition at doses of 10 mg and 25 mg. Phase III studies are ongoing to confirm these initial positive safety and efficacy findings with the 10 mg dose, and if successful, iclepertin could become the first approved pharmacotherapy used to treat CIAS.
- On May 24, 2021, Boehringer Ingelheim announced the U.S. Food and Drug Administration (FDA) had granted Breakthrough Therapy Designation (BTD) for BI 425809 for the treatment of Cognitive Impairment Associated with Schizophrenia (CIAS).
- On January 16, 2025, Boehringer Ingelheim announced top-line results from the Phase III CONNEX clinical program in cognitive impairment in adults with schizophrenia, showing primary and key secondary endpoints were not met. Boehringer Ingelheim will discontinue the long-term extension trial, CONNEX-X.
Reference:
Rosenbrock H, Desch M, Wunderlich G. Development of the novel GlyT1 inhibitor, iclepertin (BI 425809), for the treatment of cognitive impairment associated with schizophrenia. PubMed Central https://pmc.ncbi.nlm.nih.gov/articles/PMC10465677/ Accessed December 30, 2024
Development timeline for iclepertin
Further information
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