| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H23ClN2O3 |
| Molecular Weight | 410.893 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@@H](CNCCNC1=CC=CC(=C1)C2=CC=CC(=C2)C(O)=O)C3=CC=CC(Cl)=C3
InChI
InChIKey=LLDXOPKUNJTIRF-QFIPXVFZSA-N
InChI=1S/C23H23ClN2O3/c24-20-8-2-6-18(13-20)22(27)15-25-10-11-26-21-9-3-5-17(14-21)16-4-1-7-19(12-16)23(28)29/h1-9,12-14,22,25-27H,10-11,15H2,(H,28,29)/t22-/m0/s1
| Molecular Formula | C23H23ClN2O3 |
| Molecular Weight | 410.893 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.
Originator
Approval Year
Sample Use Guides
Women with OAB: Solabegron 50 mg (n=88), solabegron 125 mg (n=85), or placebo (n=85)-all twice daily-were administered.
Solabegron 125 mg produced a statistically significant difference in percent change from baseline to week 8 in incontinence episodes over 24h when compared with placebo. Solabegron 125 mg treatment also showed statistically significant reductions from baseline to weeks 4 and 8 in micturitions over 24 h and a statistically significant increase from baseline to week 8 in urine volume voided.
Route of Administration:
Oral
Solabegron (GW427353) stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human beta3-AR, with an EC50 value of 22 +/- 6 nM and an intrinsic activity 90% of isoproterenol. At concentrations of 10,000 nM, GW427353 produced a minimal response in cells expressing either beta1-ARs or beta2-ARs (maximum response <10% of that to isoproterenol).
|
|
SALT/SOLVATE -> PARENT |
|
||
|
|
TARGET -> AGONIST |
|
Showing 1 to 2 of 2 entries
