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Lodenafil

From Wikipedia, the free encyclopedia
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
  • 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
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC23H32N6O5S
Molar mass504.61g·mol−1
3D model (JSmol)
  • CCCc1c2c(c(=O)nc([nH]2)c3cc(ccc3OCC)S(=O)(=O)N4CCN(CC4)CCO)n(n1)C
  • 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
☒NcheckY(what is this?)(verify)
Lodenafil carbonate

Lodenafil(also known ashydroxyhomosildenafil,trade nameHelleva) is a drug belonging to a class of drugs calledPDE5 inhibitor,which many other erectile dysfunction drugs such assildenafil,tadalafil,andvardenafilalso belong to. Likeudenafilandavanafilit belongs to a new generation of PDE5 inhibitors.

Lodenafil is formulated as aprodrugin the form of thecarbonate esterdimer,lodenafil carbonate,which breaks down in the body to form two molecules of the active drug lodenafil. This formulation has higher oralbioavailabilitythan the parent drug.[1]

It is manufactured byCristália Produtos Químicos e FarmacêuticosinBraziland 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 theUnited Statesby theU.S. Food and Drug Administration.

See also

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References

[edit]
  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.PMID18593576.S2CID29575687.
  2. ^CristáliaArchived2015-03-15 at theWayback MachineProduct 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.PMID19040623.
  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.PMID20214718.