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Vardenafil | CAS No: 224785-90-4 | GMP-certified suppliers
A medication that treats erectile dysfunction by supporting reliable sexual function for adult patients, suitable for global sourcing across key regulated markets.
Therapeutic categories
Primary indications
- Vardenafil is indicated for the treatment of erectile dysfunction
Product Snapshot
- Vardenafil is an oral small‑molecule product supplied mainly as film‑coated and orally disintegrating tablets
- It is used for the management of erectile dysfunction
- It is approved in major regulated markets including the US, EU, and Canada
Clinical Overview
Vardenafil selectively inhibits PDE5, the predominant phosphodiesterase isoform responsible for cGMP degradation in penile smooth muscle. By reducing cGMP breakdown, it enhances smooth muscle relaxation and increases penile blood flow. Compared with sildenafil and tadalafil, vardenafil demonstrates higher PDE5 inhibitory potency, though its isoform selectivity is comparatively lower.
Following oral administration, absorption is generally rapid, and metabolism occurs primarily via CYP3A, with contributions from CYP2C9 and CYP2C19. Vardenafil is also a substrate and inhibitor of P-glycoprotein. Elimination is mainly through hepatic metabolism, with metabolites excreted in feces and urine. Pharmacokinetic parameters can be influenced by hepatic impairment, strong CYP3A inhibitors, and aging.
Safety considerations include the risk of hypotension when coadministered with nitrates or nitric oxide donors. Use is contraindicated in patients for whom sexual activity is inadvisable due to cardiovascular status. Reported adverse effects include headaches, flushing, dyspepsia, and visual disturbances. PDE5 inhibitors may rarely be associated with sudden vision or hearing loss, prolonged erections, priapism, and QT interval prolongation. Unlike some agents in its class, vardenafil has not been linked to hepatotoxicity. Evaluation as monotherapy in pulmonary arterial hypertension has been explored, although erectile dysfunction remains the primary approved indication. Notable commercial contexts include global availability under prescription brands for erectile dysfunction therapy.
For API procurement, quality assurance should emphasize verified impurity profiles, control of residual solvents, compliance with pharmacopoeial specifications, and traceable GMP manufacturing to support regulatory submission requirements.
Identification & chemistry
| Generic name | Vardenafil |
|---|---|
| Molecule type | Small molecule |
| CAS | 224785-90-4 |
| UNII | UCE6F4125H |
| DrugBank ID | DB00862 |
Pharmacology
| Summary | Vardenafil is a selective inhibitor of phosphodiesterase type 5, leading to increased intracellular cGMP levels in corpus cavernosum smooth muscle. Elevated cGMP supports nitric‑oxide–mediated smooth muscle relaxation and enhanced penile blood flow during sexual stimulation. Its activity is primarily directed at PDE5, with additional interactions reported for retinal PDE subunits. |
|---|---|
| Mechanism of action | Vardenafil inhibits cyclic guanosine monophosphate (GMP) specific phosphodiesterase type 5 (PDE5), which is responsible for the degradation of cyclic GMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The tissue concentration of cyclic GMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs), and the most abundant PDE in the human corpus cavernosum is PDE5. Therefore, the inhibition of PDE5 by vardenafil enhances erectile function by increasing the amount of cyclic GMP. |
| Pharmacodynamics | Vardenafil is a potent and selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), an enzyme responsible for the degradation of cGMP in the corpus cavernosum. The presence of cGMP in the corpus cavernosum leads to smooth muscle relaxation, an increased inflow of blood and an erection. Therefore, in patients with erectile dysfunction given vardenafil, normal sexual stimulation will increase cGMP levels in the corpus cavernosum. Without sexual stimulation and no cGMP production, vardenafil should not cause an erection. Vardenafil should not be used in men for whom sexual activity is not recommended due to their underlying cardiovascular status. There is also a risk of developing prolonged erections that last longer than 4 hours, as well as priapism. In the event of a sudden loss of vision in one or both eyes, patients should stop using vardenafil. Patients taking PDE5 inhibitors, such as vardenafil, may also develop sudden hearing loss and experience a prolonged QT interval. |
Targets
| Target | Organism | Actions |
|---|---|---|
| cGMP-specific 3',5'-cyclic phosphodiesterase | Humans | inhibitor |
| Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma | Humans | inhibitor, allosteric modulator |
| Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma | Humans | inhibitor, allosteric modulator |
ADME / PK
| Absorption | Over the recommended dose range, vardenafil has a dose-proportional pharmacokinetics profile. In healthy male volunteers given a single oral dose of 20 mg of vardenafil, maximum plasma concentrations were reached between 30 minutes and 2 hours (median 60 minutes) after oral dosing in the fasted state, and 0.00018% of the dose was detected in semen 1.5 hours after dosing. Vardenafil has a bioavailability of approximately 15%.High-fat meals cause a C<sub>max</sub> reduction of 18%-50%; however, no changes were detected in AUC or T<sub>max</sub>. |
|---|---|
| Half-life | Vardenafil and its primary metabolite (M1) have a terminal half-life of 4-5 hours. |
| Protein binding | Approximately 95% of vardenafil and its major circulating metabolite is bound to plasma proteins. Their protein binding is reversible and independent of total drug concentrations. |
| Metabolism | Vardenafil is mainly metabolized by CYP3A4 in the liver, although CYP3A5 and CYP2C isoforms also contribute to its metabolism. The major circulating metabolite, M1 (N-desethylvardenafil), results from desethylation at the piperazine moiety of vardenafil, and has a plasma concentration of approximately 26% of that of the parent compound. M1 has a phosphodiesterase selectivity profile similar to that of vardenafil and an _in vitro_ inhibitory potency for PDE5 28% of that of vardenafil. |
| Route of elimination | Vardenafil is excreted as metabolites mainly through feces and urine. Approximately 91-95% of administered oral dose is found in feces, while 2-6% of administered oral dose is found in urine. |
| Volume of distribution | Vardenafil has a steady-state volume of distribution of 208 L. |
| Clearance | Vardenafil has a total body clearance of 56 L/h. |
Formulation & handling
- Oral small‑molecule API suitable for standard tablet and ODT formulations; modest aqueous solubility may require dispersion or particle‑size optimization for rapid disintegration formats.
- Food effects are limited to reduced Cmax with high‑fat meals, so major formulation adjustments for fed/fasted variability are generally unnecessary.
- Grapefruit–CYP3A4 interaction suggests avoiding excipients or co‑formulated agents that inhibit CYP3A4 to prevent altered exposure.
Regulatory status
| Lifecycle | Most core Canadian and U.S. patents expired in 2018, with an additional U.S. patent expiring in 2023 and one extending protection to 2027, indicating a market that is largely mature with limited remaining exclusivity. With the API available across Canada, the U.S., and the EU, generic competition is likely established or emerging where patent protection has lapsed. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Vardenafil is produced by a single originator manufacturer, with a broad network of U.S.-based packagers supporting distribution. Branded and authorized generic products are present across the US, EU, and Canada, indicating established global market availability. Most key patents have expired, with one U.S. patent remaining in force until 2027, suggesting that significant generic competition is already present with some continued protection in specific markets. |
|---|
Safety
| Toxicity | Healthy male volunteers given a single dose of 120 mg of vardenafil experienced reversible back pain, myalgia and abnormal vision. Patients given vardenafil once daily over 4 weeks in single doses up to 80 mg and multiple doses up to 40 mg did not present serious adverse side effects. Cases of severe back pain were observed when 40 mg of vardenafil was administered twice daily; however patients did not present muscle or neurological toxicity. In cases of overdose, standard supportive measures should be taken as required. Renal dialysis is not expected to accelerate clearance as vardenafil is highly bound to plasma proteins and not significantly eliminated in the urine. No carcinogenic effects were detected in rats and mice given vardenafil daily for 24 months. Vardenafil was not mutagenic or clastogenic, and did not have an effect in fertility in male and female rats given up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females. |
|---|
- High-dose exposure (≥120 mg) has been associated with reversible musculoskeletal effects and transient visual disturbances
- Severe back pain noted with 40 mg twice‑daily regimens occurred without accompanying muscle or neurological toxicity
- Clearance is unlikely to be enhanced by renal dialysis due to extensive plasma‑protein binding and minimal urinary elimination
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Vardenafil is a type of Phosphodiesterase-5 inhibitors
Phosphodiesterase-5 inhibitors are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the treatment of various medical conditions. These inhibitors target the enzyme phosphodiesterase-5, which plays a crucial role in the regulation of cyclic guanosine monophosphate (cGMP) levels in the body.
By inhibiting phosphodiesterase-5, these APIs effectively increase the concentration of cGMP in certain tissues and organs, leading to several beneficial effects. One of the most well-known applications of phosphodiesterase-5 inhibitors is in the treatment of erectile dysfunction (ED). These medications, such as sildenafil, tadalafil, and vardenafil, work by enhancing the blood flow to the penile tissues, promoting and sustaining erections.
Phosphodiesterase-5 inhibitors also find applications in the treatment of pulmonary arterial hypertension (PAH). By dilating the blood vessels in the lungs, these APIs reduce the workload on the heart and improve exercise capacity in PAH patients. Furthermore, they are being explored for their potential benefits in other areas, such as the treatment of Raynaud's disease and altitude sickness.
It is important to note that phosphodiesterase-5 inhibitors should be used under medical supervision, as they can interact with other medications and have potential side effects. Common side effects include headache, flushing, nasal congestion, and gastrointestinal disturbances.
In summary, phosphodiesterase-5 inhibitors are a class of pharmaceutical APIs that are widely utilized for the treatment of erectile dysfunction and pulmonary arterial hypertension. Their ability to selectively inhibit phosphodiesterase-5 and modulate cGMP levels makes them valuable therapeutic agents in managing these conditions.
Vardenafil (Phosphodiesterase-5 inhibitors), classified under Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
Vardenafil API manufacturers & distributors
Compare qualified Vardenafil API suppliers worldwide. We currently have 7 companies offering Vardenafil API, with manufacturing taking place in 5 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aarambh Life Science | Producer | India | India | CoA, GMP | 19 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Mylan | Producer | India | Unknown | CEP, CoA | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, FDA, GMP, JDMF, KDMF, MSDS, USDMF | 64 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
When sending a request, specify which Vardenafil API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Vardenafil API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Vardenafil API
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Technical
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Regulatory
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