Lodenafil

Lodenafil (also known as 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
Clinical data
Trade namesHelleva
Pregnancy
category
  • Not for use in women
Routes of
administration		By mouth
Legal status
Legal status
  • In general: unscheduled
Identifiers
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
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H32N6O5S
Molar mass504.61 g·mol−1
3D model (JSmol)
SMILES
  • CCCc1c2c(c(=O)nc([nH]2)c3cc(ccc3OCC)S(=O)(=O)N4CCN(CC4)CCO)n(n1)C
InChI
  • InChI=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) N
  • Key:NEYKRKVLEWKOBI-UHFFFAOYSA-N N
 NY (what is this?)  (verify)
Lodenafil carbonate

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
  1. 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. S2CID 29575687.
  2. Cristália Archived 2015-03-15 at the Wayback Machine Product page. Retrieved on September 16, 2009.
  3. 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.
  4. 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.
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