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cizolirtine
- Development stage
- Discontinued
- Lead developer
- Esteve
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Cizolirtine is a small molecule pyrazole derivative originally developed by Esteve Pharmaceuticals for the treatment of various pain conditions and urinary incontinence secondary to overactive bladder. Its mechanism of action involves the modulation of neuropeptide release, specifically inhibiting the presynaptic release of substance P (SP) and calcitonin gene-related peptide (CGRP) at the spinal cord level. This inhibitory effect is mediated through an alpha-2 adrenoceptor-dependent pathway. Clinical development reached Phase II and Phase III for indications including neuropathic pain, renal colic, cancer pain, and diabetic neuropathy, as well as overactive bladder. However, the global research and development for cizolirtine has been discontinued.
- Other names
- cizolirtine citrate
02
Targets
CGRP (Calcitonin gene-related peptide)SP (Substance P)ADRA2A (α2A)
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