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OPC-51803
- Development stage
- Discontinued
- Lead developer
- Otsuka Holdings
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
OPC-51803 is an orally active small molecule and the first nonpeptide selective agonist of the vasopressin V2 receptor. It was developed for the treatment of conditions characterized by excessive urination and frequent micturition such as hypothalamic diabetes insipidus, nocturnal enuresis (bedwetting), polyuria (excessive urine production), nocturnal polyuria (nighttime overproduction of urine), and some forms of urinary incontinence. Mechanistically, OPC-51803 acts as a selective agonist at the vasopressin V2 receptor (AVPR2), leading to increased antidiuretic activity via stimulation of cyclic AMP production in renal collecting duct cells. This results in enhanced water reabsorption and reduced urine output. The drug was originally developed by Otsuka Pharmaceutical but its development has been discontinued for all indications[1][2][3][4][5][6].
- Other names
- 192514-54-8HY-116567HY116567HY 116567CS-0065910CS0065910CS 0065910NS00069347NS-00069347NS 00069347Q27088207Q-27088207Q 27088207BDBM50117486BDBM-50117486BDBM 50117486AKOS040749086AKOS-040749086AKOS 040749086
02
Targets
AVPR1B (Vasopressin V1b Receptor)AVPR1A (Arginine vasopressin receptor 1A)AVPR2 (Arginine vasopressin V2 receptor)
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