Overactive bladder treatments in early phase clinical trials

• EDWARDS G, HENSHAW M, MILLER M, WESTON AH: Comparison of the effects of several potassium-channel openers on rat bladder and rat portal vein in vitro. Br. J. Pharmacol. (1991) 102:679-686.
   PubMed Web of Science ®Google Scholar
• BARRAS M, VAN DER GRAF PH, CHRISTOPH P, ITZCHAK A: Relaxant efficacy of potassium channel openers in rabbit isolated bladder and mesenteric artery. Eur. J. Urol. (1996) 30(Suppl. 2):240 (Abstract).
   Google Scholar
• HEDLUND H, ANDERSSON K-E, MATTIASSON A: Effects of pinacidil on detrusor instability in men with outlet obstruction. J. Urol. (1991) 146:1345-1347.
   PubMed Web of Science ®Google Scholar
• KOMERSOVA K, ROGERSON JW, CONWAY EL et al.: The effect of levcromakalim (BRL 38227) on bladder function in patients with high spinal cord lesions. Br. J. Pharmacol. (1995) 39:207-209.
   Web of Science ®Google Scholar
• MAZZUCCO R: American Urological Association – 96th Annual Meeting. 2-7 June 2001, Anaheim, CA, USA. IDrugs (2001) 4(8):892-895.
   PubMedGoogle Scholar
• CONTRAFOURIS Y: Medicinal Chemistry – XVIIth International Symposium. IDrugs (2002) 5(10):961-963.
   PubMedGoogle Scholar
• PEREZ-MEDRANO A, KORT ME, GREGG RJ et al.: Buckner design and synthesis of aminal-containing ATP-sensitive potassium channel openers for the treatment of bladder overactivity. 224^th American Chemical Society Meeting, Boston, USA (18 – 22 August 2002).
   Google Scholar
• JAEHNE G, LANG HJ, GLOMBIK H, GEISEN K et al.: In vivo anorectic activity of substituted tetrahydro-indeno[1,2-d]thiazols. 224^th American Chemical Society Meeting, Boston, MA, USA (18 – 22 August 2002).
   Google Scholar
• TURNER SC, CARROLL WA, WHITE TK et al.: The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles. Bioorg. Med. Chem. Lett. (2003) 13(12):2003-2007.
   PubMed Web of Science ®Google Scholar
• CARROLL WA, ALTENBACH RJ, BAI H et al.: Synthesis and structure–activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent KATP opener that selectively inhibits spontaneous bladder contractions. J. Med. Chem. (2004) 47(12):3163-3179.
   PubMed Web of Science ®Google Scholar
• PEREZ-MEDRANO A, BUCKNER SA, COGHLAN MJ et al.: Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder. Bioorg. Med. Chem. Lett. (2004) 14(2):397-400.
   PubMed Web of Science ®Google Scholar
• PEREZ-MEDRANO A, BUCKNER SA, COGHLAN MJ et al.: Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder. Bioorg. Med. Chem. Lett. (2004) 14(2):397-400.
   PubMed Web of Science ®Google Scholar
• TURNER SC, CARROLL WA, WHITE TK et al.: The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure–activity relationships of 2-amino-4-azaindoles. Bioorg. Med. Chem. Lett. (2003) 13(12):2003-2007.
   PubMed Web of Science ®Google Scholar
• JENSEN BS, KJAER K, CHRISTOPHENSEN P: NS309: a novel low nanomolar potency activator of voltage-independent, Ca2+-activated K+ channels. Society of Neuroscience Abstracts (2003):33.
   Google Scholar
• WICKENDEN A: SRI's Second International Symposium on Ion Channels in Drug Discovery and Development, Princeton, NJ, USA, 24 – 25 October (2002).
   Google Scholar
• HEWAWASAM P, ERWAY M, THALODY G et al.: The synthesis and structure–activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones: a new class of calcium-dependent, large conductance, potassium (Maxi-K) channel opener targeted for urge urinary incontinence. Bioorg. Med. Chem. Lett. (2002) 12(7):1117-1120.
   PubMed Web of Science ®Google Scholar
• KONTANI H, JINKAWA M, SHIRAOYA C, NAGASHIMA A: Effect of K+ channel openers, KRN2391 and Kil769, and nitroglycerine on the urinary tract of rats in vivo. Jpn J. Pharmacol. (1999) 80(2):143-153.
   PubMedGoogle Scholar
• TANAKA M, SASAKI Y, HUKUI T et al.: A novel pyrrole derivative, NS-8, activates the Ca2+ sensitive K+-channels and suppresses micturition reflex in rats. J. Urol. (1998) 159(Suppl. 5).
   Web of Science ®Google Scholar
• BRIONI JD, MORELAND RB: American Urological Association – 95th Annual Meeting. IDrugs (2000) 3(7):762-765.
   PubMedGoogle Scholar
• TANAKA M, SASAKI Y, KIMURA Y, FUKUI T, HAMADA K, UKAI Y: A novel pyrrole derivative, NS-8, suppresses the rat micturition reflex by inhibiting afferent pelvic nerve activity. BJU Int. (2003) 92(9):1031-1036.
   Google Scholar
• LU SH, YAMAGATA T, ATSUKI K et al.: Effect of KW-7158, a putative afferent nerve inhibitor, on bladder and vesico-vascular reflexes in rats. Brain Res. (2002) 946(1):72-78.
   Google Scholar
• CHAPPLE C, PATRONEVA A, RAINES RS: Effect of an ATP-sensitive potassium channel opener in subjects with overactive bladder: a randomized, double-blind, placebo-controlled study (ZD0947IL/0004). Eur. Urol. (2006) 49:879-886.
   PubMed Web of Science ®Google Scholar
• COCKAYNE DA, HAMILTON SG, ZHU QM et al.: Urinary bladder hyporeflexia and reduced pain-related behaviour in P2X3-deficient mice. Nature (2000) 407:1011-1015.
   PubMed Web of Science ®Google Scholar
• VLASKOVSKA M, KASAKOV L, RONG W et al.: G.P2X3 knock-out mice reveal a major sensory role for urothelially released ATP. J. Neurosci. (2001) 21:5670-5677.
   PubMed Web of Science ®Google Scholar
• KIBBLE A: Division of medicinal chemistry – P2 nucleotide receptors. IDrugs (2000) 3(11):1270-1271.
   Google Scholar
• EMONDS-ALT X, PROIETTO V, STEINBERG R et al.: SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)-phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]-4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. J. Pharmacol. Exp. Ther. (2002) 303(3):1171-1179.
   PubMed Web of Science ®Google Scholar
• MICHEL MC: Lower urinary tract disorders – Ray Fuller Symposium, physiology, pharmacology and therapeutic approaches. IDrugs (2002) 5:792-796.
   Google Scholar
• GREEN SA, ALON A, IANUS J, MCNAUGHTON KS, TOZZI CA, REISS TF: Efficacy and safety of a neurokinin-1 receptor antagonist in postmenopausal women with overactive bladder with urge urinary incontinence. J. Urol. (2006) 176:2535-2540.
   PubMed Web of Science ®Google Scholar
• SUM FW, WONG V, HAN S, LARGIS E, MULVEY R, TILLETT J: Cyclic amine sulfonamides as linkers in the design and synthesis of novel human b(3) adrenergic receptor agonists. Bioorg. Med. Chem. Lett. (2003) 13(13):2191-2194.
   PubMed Web of Science ®Google Scholar
• CELLEK S, THANGIAH R, BASSIL AK et al.: β3 adrenoceptor agonism decreases motility and induces anti-hyperalgesia: a novel target for IBS. Gastroenterology (2006) 130(4 Suppl. 2).
   Google Scholar
• WIBBERLY A, WESTFALL TD, RIEDEL ES et al.: GW427353 (solabegron), a b3 adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. Abstracts of the American Urological Association Annual Meeting, San Antonio, Texas, USA (21 – 26 May 2005). J. Urol. (2005) 173(Suppl. 4):1-467.
   PubMedGoogle Scholar
• YAMAZAKI Y, TATEMICHI S, MARUYAMA I et al.: Characterization of KUC-7483 and its active metabolite, KUC-7322, a selective β3-adrenoceptor agonist, on bladder function in rats. Neurourol. Urodyn. (2002) 21(4):405-406.
   Google Scholar
• ANDERSSON KE: Treatment of overactive bladder: other drug mechanisms. Urology (2000) 55:51-57.
   PubMed Web of Science ®Google Scholar
• CRESCIOLI C, MORELLI A, ADORINI L et al.: Human bladder as a novel target for vitamin D receptor ligands. J. Endocrinol. Metab. (2004) 90(2):962-972.
   PubMed Web of Science ®Google Scholar
• MORELLI A, VIGNOZZI L, FILIPPI S et al.: BXL-628, a vitamin D receptor antagonist effective in benign prostatic hyperplasia treatment, prevents RhoA activation and inhibits RhoA/Rho kinase signaling in rat and human bladder. Prostate (2006) (In Press).
   Google Scholar
• HUFF FJ: Preliminary evaluation of besipirdine for the treatment of Alzheimer's disease. Besipirdine study group. Ann. NY Acad. Sci. (1996) 777:410-414.
   Google Scholar
• BRUBAKER L, CHAPPLE C, COYNE KS, KOPP Z: Patient-reported outcomes in overactive bladder: importance for determining clinical effectiveness of treatment. Urology (2006) 68(Suppl. 2):3-8.
   PubMed Web of Science ®Google Scholar
• VOELKER R: International group seeks to dispel incontinence “taboo”. JAMA (1998) 280:951.
   PubMed Web of Science ®Google Scholar
• CHAPPLE C: Interview with Chris Chapple. Overactive bladder: tackling the problem. Eur. Urol. (2006) 49(5):921-923.
   PubMed Web of Science ®Google Scholar
• OUSLANDER JG: Management of overactive bladder. N. Engl. J. Med. (2004) 350(8):786-799.
   PubMed Web of Science ®Google Scholar

Websites

• http://www.apogepha.de/en/ Apogepha website (2007).
   Google Scholar
• http://www.recordati.it Recordati website (2007).
   Google Scholar
• http://www.tanabe.co.jp Tanabe Seiyaku Co. Ltd website (2007).
   Google Scholar
• http://www.astellas.com Astellas Pharma, Inc. website (2007).
   Google Scholar
• http://www.dynogenpharma.com Dynogen Pharmaceuticals, Inc. website (2007).
   Google Scholar
• http://www.nicox.com/ NiCox website (2007).
   Google Scholar
• http://www.bioxell.com/ Bioxell website (2007).
   Google Scholar