Lodenafil
{{Drugbox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 451225761 | IUPAC_name = 5-(2-Ethoxy-5-{[4-(2-hydroxyethyl)-1-piperazinyl]sulfonyl}phenyl)-1-methyl-3-propyl-1,4-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | image = Lodenafil structure.png
| tradename = Helleva | pregnancy_category = Not for use in women | legal_status = Unscheduled | routes_of_administration = Oral
| bioavailability = | metabolism = | excretion =
| CAS_number_Ref = 
| CAS_number = 398507-55-6
| DrugBank =
| ChemSpiderID_Ref = 
| C=23 | H=32 | N=6 | O=5 | S=1
| molecular_weight = 504.602 g/mol
| PubChem = 4742795
| ChemSpiderID = 3929995
| smiles = CCCc1c2c(c(=O)nc([nH]2)c3cc(ccc3OCC)S(=O)(=O)N4CCN(CC4)CCO)n(n1)C
| StdInChI = 1S/C23H32N6O5S/c1-4-6-18-20-21(27(3)26-18)23(31)25-22(24-20)17-15-16(7-8-19(17)34-5-2)35(32,33)29-11-9-28(10-12-29)13-14-30/h7-8,15,30H,4-6,9-14H2,1-3H3,(H,24,25,31)
| StdInChIKey = NEYKRKVLEWKOBI-UHFFFAOYSA-N
}}
Lodenafil (Hydroxyhomosildenafil, trade name Helleva) is a drug belonging to a class of drugs called PDE5 inhibitor, which many other erectile dysfunction drugs such as sildenafil, tadalafil, and vardenafil also belong to. Like udenafil and avanafil it belongs to a new generation of PDE5 inhibitors.
Lodenafil is formulated as a prodrug in the form of the carbonate ester dimer, lodenafil carbonate, which breaks down in the body to form two molecules of the active drug lodenafil. This formulation has higher oral bioavailability than the parent drug.[1]
It is manufactured by Cristália Produtos Químicos e Farmacêuticos in Brazil and sold there under the brand-name Helleva.[2]
It has undergone Phase III clinical trials,[3][4] but is not yet approved for use in the United States by the U.S. Food and Drug Administration.
See also
References
- ^ Toque HA, Teixeira CE, Lorenzetti R, Okuyama CE, Antunes E, De Nucci G (September 2008). "Pharmacological characterization of a novel phosphodiesterase type 5 (PDE5) inhibitor lodenafil carbonate on human and rabbit corpus cavernosum". European Journal of Pharmacology. 591 (1–3): 189–95. doi:10.1016/j.ejphar.2008.06.055. PMID 18593576.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Cristália Product page. Retrieved on September 16, 2009.
- ^ Glina S, Toscano I, Gomatzky C, de Góes PM, Júnior AN, Claro JF, Pagani E (February 2009). "Efficacy and tolerability of lodenafil carbonate for oral therapy in erectile dysfunction: a phase II clinical trial". The Journal of Sexual Medicine. 6 (2): 553–7. doi:10.1111/j.1743-6109.2008.01079.x. PMID 19040623.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Glina S, Fonseca GN, Bertero EB, Damião R, Rocha LC, Jardim CR, Cairoli CE, Teloken C, Torres LO, Faria GE, da Silva MB, Pagani E (February 2010). "Efficacy and Tolerability of Lodenafil Carbonate for Oral Therapy of Erectile Dysfunction: A Phase III Clinical Trial". The Journal of Sexual Medicine. 7 (5): 1928–1936. doi:10.1111/j.1743-6109.2010.01711.x. PMID 20214718.
{{cite journal}}: CS1 maint: multiple names: authors list (link)
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