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Norgestimate | CAS No: 35189-28-7 | GMP-certified suppliers
A medication that supports hormonal contraception and helps manage moderate acne in eligible females, serving key needs in reproductive health and dermatologic care.
Therapeutic categories
Primary indications
- Norgestimate is formulated with [ethinylestradiol] as a combined oral contraceptive
- It can also be given with low dose ethinylestradiol for contraception as well as the treatment of moderate acne vulgaris in women ≥15 years old
Product Snapshot
- Oral small‑molecule formulation supplied as coated tablets and kits for combined use with ethinylestradiol
- Used for contraception and for adjunct treatment of moderate acne vulgaris in appropriate female populations
- Approved in the US and Canada, with additional investigational status noted in some records
Clinical Overview
Clinically, norgestimate provides contraceptive efficacy primarily through suppression of ovulation. Its acne benefit reflects reduction of circulating free testosterone when used with ethinylestradiol. Approved products include multiple combined oral contraceptive brands that incorporate norgestimate as the progestin component.
Pharmacologically, norgestimate functions as a progestational agent that diminishes hypothalamic gonadotropin-releasing hormone pulsatility. This results in decreased secretion of follicle-stimulating hormone and luteinizing hormone, preventing follicular maturation and ovulation. Additional suppression of the hypothalamo-pituitary axis reduces ovarian androgen synthesis. Induction of sex hormone binding globulin further lowers free testosterone concentrations, contributing to reduced sebaceous gland stimulation.
The compound is considered a prodrug that undergoes metabolic activation after oral administration. Norgestimate and its active metabolites are processed through hepatic pathways, with evidence of involvement of CYP3A and other cytochrome P450 isoforms based on substrate classifications. It exhibits predictable oral bioavailability within the context of combined formulations, although specific kinetic parameters vary by product.
Safety considerations include the known class effects of combined hormonal contraceptives, such as risk of thromboembolic events, hypertension, hepatic effects, and glucose and lipid alterations. Headache, mood changes, and breakthrough bleeding may occur. The therapeutic index is wide, and clinically significant overdose is uncommon, but patient selection and monitoring should follow contraceptive risk assessment standards.
For API procurement, suppliers should provide evidence of GMP-compliant production, control of stereochemistry and impurity profiles, and robust stability data to support formulation development and regulatory submissions across global markets.
Identification & chemistry
| Generic name | Norgestimate |
|---|---|
| Molecule type | Small molecule |
| CAS | 35189-28-7 |
| UNII | NKX8DN6TY9 |
| DrugBank ID | DB00957 |
Pharmacology
| Summary | Norgestimate is a progestin that acts primarily through progesterone receptors to suppress hypothalamic GnRH pulsatility, leading to reduced FSH and LH secretion and inhibition of ovulation. It also increases sex hormone–binding globulin and decreases androgen activity, lowering free testosterone levels. These endocrine effects support its use in combined oral contraceptives and in regimens targeting androgen‑responsive acne. |
|---|---|
| Mechanism of action | Progesterone analogs like norgestimate decrease the frequency of gonadotropin releasing hormone pulses from the hypothalamus, decreasing follicle stimulating hormone and luteinizing hormone.These actions prevent ovulation. Norgestimate suppresses the hypothalamo-pituitary-axis, reducing androgen synthesis.It also induces production of sex hormone binding globulin, which decreases free testosterone.These actions together result in less testosterone being available to stimulate sebaceous glands, resulting in effective treatment of some forms of acne. |
| Pharmacodynamics | Norgestimate is a progestin that suppresses ovulation for contraception and reduces free testosterone to treat moderate acne vulgaris.The therapeutic index is wide as overdoses are rare.Patients should be counselled regarding the risk of vascular problems, liver disease, hypertension, metabolic effects, headaches, and bleeding irregularities. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Progesterone receptor | Humans | agonist |
| Estrogen receptor alpha | Humans | agonist |
| Androgen receptor | Humans | partial agonist |
ADME / PK
| Absorption | Oral norgestimate has a T<sub>max</sub> of 0.5-2h. On day 21 of cycle 3, 17-desacetylnorgestimate reaches a C<sub>max</sub> of 1.82ng/mL, with a T<sub>max</sub> of 1.5h, and an AUC of 16.1h\*ng/mL.At the same time, norgestrel reaches a C<sub>max</sub> of 2.79ng/mL, with a T<sub>max</sub> of 1.7h, and an AUC of 49.9h\*ng/mL. |
|---|---|
| Half-life | Norgestimate is rapidly deacetylated.The active metabolites of norgestimate, 17-desacetyl norgestimate, has a half life of 12-30h,while norgestrel has a half life of 36.4±10.2h. |
| Protein binding | 17-desacetylnorgestimate is 97.2% bound to albumin and Norgestrel is >97% protein bound, including 92.5% bound to sex hormone binding globulin. |
| Metabolism | Norgestimate is rapidly deacetylated to the active 17-desacetylnorgestimate, which is deoximated to the active norgestrel.17-desacetylnorgestimate is metabolized to a number of undefined hydroxylated metabolites, mainly by CYP3A4 and to a lesser extend by CYP2B6 and CYP2C9.Norgestrel is O-glucuronidated by UGT1A1 or oxidized to a number of undefined hydroxylated metabolites by CYP3A4. |
| Route of elimination | Norgestimate is 45-49% eliminated in urine and 16-49% eliminated in feces.Unchanged norgestimate is not detected in urine. |
| Volume of distribution | Data regarding the volume of distribution of norgestimate are not readily available. |
| Clearance | Data regarding the clearance of norgestimate is not readily available. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity support conventional oral tablet formulations using solubilizers or dispersion strategies to ensure consistent dissolution.
- Solid, lipophilic steroid ester is chemically stable under typical dry conditions but benefits from protection against hydrolysis during processing and storage.
- Food has minimal impact on absorption, allowing flexible administration and simplifying formulation considerations for oral fixed‑dose combination kits.
Regulatory status
| Lifecycle | The API’s primary U.S. patents expired between 2012 and 2020, indicating that market exclusivity has concluded. With products marketed in the United States and Canada, the ingredient is now in a mature, post‑exclusivity phase. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Norgestimate is supplied by multiple manufacturers and repackagers, indicating that originator exclusivity has transitioned to a broad generic supply base. Branded products appear primarily in the US and Canada, with limited evidence of wider global distribution in the provided data. Key US patents expired between 2012 and 2020, supporting the presence of established generic competition. |
|---|
Safety
| Toxicity | Data regarding overdoses of norgestimate are rare.However, the majority of patients overdosing on oral contraceptives do not become seriously ill.Treat overdoses with symptomatic and supportive care. |
|---|
- Reported overdose cases are uncommon and generally exhibit low clinical severity, but monitoring for nonspecific adverse effects is standard in handling concentrated material
- Management of acute exposure is supportive
- No specific antidote is identified in the literature
Norgestimate is a type of Contraceptives
Contraceptives are a vital subcategory within the pharmaceutical active pharmaceutical ingredient (API) sector. These substances play a crucial role in preventing unwanted pregnancies and providing individuals with reliable birth control options. Contraceptives are designed to interfere with the natural processes of fertilization and implantation, thereby reducing the chances of conception.
APIs used in contraceptives exhibit specific mechanisms of action to ensure effective contraception. These may include inhibiting ovulation, altering cervical mucus consistency, or impeding sperm mobility and viability. By utilizing targeted APIs, contraceptive manufacturers can develop diverse products, including oral contraceptive pills, contraceptive patches, intrauterine devices (IUDs), and contraceptive injections.
The pharmaceutical industry places utmost importance on the quality, safety, and efficacy of contraceptive APIs. Stringent regulations govern their production, ensuring adherence to Good Manufacturing Practices (GMP) and quality control standards. Additionally, pharmaceutical companies invest in comprehensive research and development to enhance contraceptive formulations, minimize side effects, and improve user compliance.
Contraceptives are widely utilized across the globe, offering individuals the ability to make informed choices regarding family planning and reproductive health. With increasing awareness and evolving societal norms, the demand for effective contraceptives continues to grow. Pharmaceutical API manufacturers play a pivotal role in meeting this demand by producing high-quality contraceptive APIs that provide reliable and accessible birth control options to individuals worldwide.
Norgestimate (Contraceptives), 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.
Norgestimate API manufacturers & distributors
Compare qualified Norgestimate API suppliers worldwide. We currently have 5 companies offering Norgestimate 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 |
|---|---|---|---|---|---|
| Expert Synthesis Solution... | Producer | Canada | Canada | CoA | 1 products |
| Gedeon Richter | Producer | Hungary | Unknown | CEP, CoA, FDA, GMP, USDMF | 48 products |
| Industriale Chimica | Producer | Italy | Unknown | CEP, CoA, GMP, USDMF | 33 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
When sending a request, specify which Norgestimate 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 Norgestimate 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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Technical
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Regulatory
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