| Clinical data | |
|---|---|
| Other names | PT100114; TCAP-1 |
| Routes of administration | Subcutaneous injection [1] [2] |
| Drug class | Corticotropin-releasing hormone (CRH) inhibitor |
PT-00114, also known as TCAP-1, is a corticotropin-releasing hormone (CRH) inhibitor which is under development for the treatment of generalized anxiety disorder, major depressive disorder, opioid-related disorders, post-traumatic stress disorder (PTSD), and mood disorders. [1] [3] [2] It is taken by subcutaneous injection. [1] [2] The drug is a synthetic analogue of the teneurin C-terminal associated peptides (TCAP) and is a 41-amino acid peptide. [2] [4] [5] It has been reported to produce anxiolytic-like effects in animals, among other effects. [4] PT-00114 is under development by Protagenic Therapeutics and Charles River Laboratories. [1] As of August 2025, it is in phase 1/2 clinical trials for generalized anxiety disorder, major depressive disorder, opioid-related disorders, and PTSD and is in phase 1 trials for mood disorders. [1] [3] It is or was also under development for the treatment of other anxiety and depressive disorders as well as of impulse control disorders and neurodegenerative disorders, but no recent development has been reported for these indications. [1]
PT-00114 (TCAP-1) is under development for the treatment of mood disorders, substance abuse and addiction, opioid addiction and other neurodegenerative disorders including post-traumatic stress disorder (PTSD), treatment resistant depression, generalized anxiety disorder and unspecified CNS disorders. It is a synthetic form of the natural peptide sequence TCAP-1. It acts by targeting corticotropin-releasing hormone (CRH). It is developed based on peptide technology. It was also under development for the treatment of spinal cord injuries, ischemia and trauma. It is administered by subcutaneous route.
[...] Recently, synthetic TCAP-1 (serial #: PT00114) has been found to modulate several behavioural and neuronal effects of CRF in a primarily, though not exclusively (Tan et al., 2008), inhibitory manner. For example, 5 days of intravenous TCAP-1 injections decreased CRF-induced anxiety in the open field and elevated plus maze (Al Chawaf et al., 2007), and 5 days of i.c.v. TCAP-1 injections blocked CRF-induced increases in acoustic startle responses (Tan et al., 2008). Furthermore, acute i.c.v. injections of TCAP-1 attenuated CRFinduced expression of c-fos, a widely used marker of neuronal activation (Curran and Morgan, 1995), in the hippocampus, amygdala and other limbic brain regions (Tan et al., 2009). Based on these and similar findings, it has been proposed that TCAP in the CNS may serve as an endogenous neuropeptide to attenuate the actions of CRF and, thereby, influence behaviour (Lovejoy et al., 2009). [...]
PT00114, a 41-amino-acid synthetic peptide, holds promise in treating various neuro-psychiatric conditions, including depression, anxiety, and PTSD. It operates with a novel mechanism, mirroring the active part of the natural brain hormone TCAP, thereby reducing circulating cortisol levels.
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