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Desmopressin | CAS No: 16679-58-6 | GMP-certified suppliers
A medication that addresses nocturia from nocturnal polyuria, manages central diabetes insipidus and transient polyuria, and supports perioperative hemostasis in mild hemophilia A or type I von Willebrand disease.
Therapeutic categories
Primary indications
- Indicated for the treatment of nocturia due to nocturnal polyuria in adults who awaken at least 2 times per night to void (intranasal)
- Indicated as antidiuretic replacement therapy in the management of central cranial diabetes insipidus and for management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region (intranasal/parenteral)
- Indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5% or mild to moderate classic von Willebrand's Disease (Type I) with factor VIII levels greater than 5% during surgical procedures and postoperatively to maintain hemostasis (parenteral)
Product Snapshot
- Desmopressin is a synthetic peptide available as injectable, intranasal spray, and oral tablet formulations
- It is used for antidiuretic management in nocturnal polyuria and central diabetes insipidus, and for perioperative hemostatic support in mild hemophilia A and type I von Willebrand disease
- It is approved in the US and Canada
Clinical Overview
Pharmacologically, desmopressin acts as a selective V2 receptor agonist in the distal nephron and collecting ducts. Receptor activation stimulates adenylyl cyclase, increases intracellular cyclic AMP, and promotes insertion of aquaporin water channels into the apical membrane, enhancing water reabsorption and reducing urine volume. Compared with vasopressin, desmopressin demonstrates much lower pressor activity. Intranasal administration produces roughly one‑tenth the antidiuretic effect of an equivalent parenteral dose.
Absorption and bioavailability vary by route, with intranasal formulations demonstrating lower systemic exposure than oral or parenteral products. Distribution is primarily extracellular, and the peptide is metabolized by peptidases with renal elimination of active and inactive components. The prolonged half‑life relative to vasopressin supports dosing intervals appropriate for chronic management of nocturnal polyuria or diabetes insipidus.
Safety considerations focus on hyponatremia and water retention, particularly in elderly patients or when fluid intake is not appropriately restricted. Other risks include headache, nasal irritation for intranasal products, and rare thrombotic events in hemostatic use. Formulations containing desmopressin acetate are marketed globally, with Nocdurna representing a sublingual option approved for adult nocturia due to nocturnal polyuria.
For API procurement, sourcing should ensure control of peptide integrity, stereochemistry, residual solvents, and microbiological quality, with verified compliance to pharmacopeial monographs and consistent lot‑to‑lot purity.
Identification & chemistry
| Generic name | Desmopressin |
|---|---|
| Molecule type | Small molecule |
| CAS | 16679-58-6 |
| UNII | ENR1LLB0FP |
| DrugBank ID | DB00035 |
Pharmacology
| Summary | Desmopressin is a selective agonist of renal V2 receptors, activating adenylyl cyclase and promoting aquaporin insertion in collecting duct cells to enhance water reabsorption and reduce urine output. It mimics endogenous antidiuretic hormone with minimal pressor activity and also increases circulating factor VIII and von Willebrand factor in susceptible patients. Minor activity at V1a and V1b receptors is present but not central to its therapeutic effects. |
|---|---|
| Mechanism of action | Upon binding of desmopressin to V2 receptors in the basolateral membrane of the cells of the distal tubule and collecting ducts of the nephron, adenylyl cyclase is stimulated. The resulting intracellular cascades in the collecting duct lead to increased rate of insertion of water channels, called aquaporins, into the lumenal membrane and enhanced the permeability of the membrane to water . |
| Pharmacodynamics | By mimicking the actions of endogenous ADH, desmopressin acts as a selective agonist of V2 receptors expressed in the renal collecting duct (CD) to increase water re-absorption and reduce urine production. Desmopressin has been shown to be more potent than ADH in increasing plasma levels of factor VIII activity in patients with hemophilia and von Willebrand's disease Type I . Desmopressin demonstrates markedly diminished pressor activity. Desmopressin administered intranasally has an antidiuretic effect about one-tenth that of an equivalent dose administered by injection . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Vasopressin V2 receptor | Humans | agonist |
| Vasopressin V1a receptor | Humans | |
| Vasopressin V1b receptor | Humans |
ADME / PK
| Absorption | Following nasal spray administration of 0.83 mcg and 1.66 mcg, median time to peak plasma concentrations (Tmax) was 0.25 and 0.75 hour, respectively [FDA Label]. The peak plasma concentration was approximately 4.00 (± 3.85) pg/mL and 9.11 (± 6.90) pg/mL, respectively [FDA Label]. The bioavailability of 1.5 mg/mL desmopressin administered by the intranasal route was between 3.3 and 4.1% . The absolute bioavailability of orally administered desmopressin varies between 0.08% and 0.16% where the mean maximum plasma concentration is reached within 2 hours . |
|---|---|
| Half-life | Following an intranasal dose of 1.66 mcg of desmopressin, the median apparent terminal half-life was 2.8 hours [FDA Label]. Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment [FDA Label]. The oral terminal half life of desmopressin ranges from 2 to 3.11 hours . |
| Protein binding | Following radioiodination (125I) in the N-terminal, the fraction of plasma protein binding of desmopressin was reported to be 17.3 ± 1.5% in a pharmacokinetic study involving healthy subjects . |
| Metabolism | In vitro, in human liver microsome preparations, it has been shown that no significant amount of desmopressin is metabolised in the liver and thus human liver metabolism in vivo is not likely to occur . |
| Route of elimination | Desmopressin is mainly excreted in the urine. About 65% of the amount of desmopressin absorbed after oral administration could be recovered in the urine within 24 hours . |
| Volume of distribution | The distribution volume of orally administered desmopressin is 0.2 – 0.32 l/kg . It is not reported to cross the blood-brain barrier. |
Formulation & handling
- Desmopressin is a peptide‑derived small molecule with very low logP, requiring aqueous parenteral systems and stabilization against hydrolysis and adsorption to surfaces.
- Oral and sublingual forms face limited permeability and enzymatic degradation, so formulations typically rely on rapid‑dissolution matrices and protection from moisture.
- Nasal and inhalation products need attention to peptide stability in solution, preservative compatibility, and droplet/actuation consistency to ensure reliable absorption.
Regulatory status
| Lifecycle | The API shows a mature lifecycle in Canada, where key patents have expired, while in the United States limited protection remains in place through a 2030 patent. Overall, the product is marketed in both regions with most exclusivities concluded except for the remaining US patent. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The desmopressin supply landscape includes an originator and multiple established manufacturers, with numerous packagers supporting secondary operations across North America. Branded products are present in the US and Canada, alongside several distributed brand variants. Multiple patents have already expired in both markets, and with remaining protection extending only to 2030 for select US claims, the product class shows existing and continued space for generic competition. |
|---|
Safety
| Toxicity | Intravenous TDLo in humans is reported to be 0.3 µg/kg/10M [MSDS]. Desmopressin is associated with hyponatremia in case of overdose, which may require temporary or permanent discontinuation of the therapy depending on severity. The effects of hyponatremia include seizure, altered mental status (confusion, drowsiness or continuing headache), cardiac arrhythmias and worsening edema. Other signs of overdose may include oliguria and rapid weight gain due to fluid retention [FDA Label]. In case of overdose, reduce the dose or frequency of drug administration, or discontinue use if appropriate. Assessment of serum sodium and initiation of appropriate medical treatment is recommended. |
|---|
- Very low intravenous TDLo in humans (0
- 3 µg/kg/10 min) indicates high potency
- Handle with controls that minimize risk of occupational exposure
Desmopressin is a type of Urological agents
Urological agents are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used for the treatment of various urological disorders. These agents encompass a wide range of drugs that target the urinary system, including the kidneys, bladder, ureters, and urethra.
One common type of urological agent is the alpha-blockers. These medications work by relaxing the smooth muscles in the prostate gland, bladder neck, and urethra, thereby improving urine flow and relieving symptoms associated with benign prostatic hyperplasia (BPH). Alpha-blockers are frequently prescribed to alleviate urinary retention and reduce the urgency and frequency of urination.
Another important class of urological agents is the antimuscarinics. These drugs act by blocking the action of acetylcholine, a neurotransmitter responsible for the contraction of the bladder muscle. By inhibiting these contractions, antimuscarinics help to reduce overactive bladder symptoms, such as frequent urination, urgency, and urge incontinence.
Additionally, urological agents may include medications for the treatment of urinary tract infections (UTIs), such as antibiotics targeting specific bacteria commonly responsible for UTIs. These antibiotics work by inhibiting bacterial growth and eradicating the infection.
The development of urological agents plays a crucial role in improving the quality of life for patients suffering from urological conditions. These pharmaceutical APIs offer effective therapeutic options to manage symptoms and address the underlying causes of urological disorders. By targeting specific mechanisms within the urinary system, urological agents offer precise and targeted treatment approaches. It is essential for healthcare professionals to stay updated on the latest advancements in urological agents to ensure optimal patient care.
Desmopressin (Urological agents), 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.
Desmopressin API manufacturers & distributors
Compare qualified Desmopressin API suppliers worldwide. We currently have 8 companies offering Desmopressin API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| BCN Peptides | Producer | Spain | Spain | CEP, CoA, FDA, GMP, USDMF | 13 products |
| Chengdu Shengnuo Biopharm... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 33 products |
| Hemmo Pharma | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 13 products |
| Hybio Pharmaceutical | Producer | China | China | CoA, USDMF | 8 products |
| Hybio Pharmaceutical Co L... | Producer | China | China | BSE/TSE, CEP, CoA, FDA, GMP, MSDS | 34 products |
| Mylan | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 201 products |
| Polypeptide Labs | Producer | Sweden | Sweden | CEP, CoA, FDA, GMP, JDMF, USDMF | 21 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
When sending a request, specify which Desmopressin 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 Desmopressin 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.
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