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Isotretinoin | CAS No: 4759-48-2 | GMP-certified suppliers
A medication that treats severe recalcitrant nodular acne in patients aged 12 and older, supporting reliable dermatologic therapy requirements for regulated markets.
Therapeutic categories
Primary indications
- Isotretinoin is indicated to treat severe recalcitrant nodular acne and patients ≥12 years enrolled in the iPLEDGE program
- [Label,L6579]
Product Snapshot
- Oral and topical small‑molecule formulations are available, including multiple capsule presentations and dermatologic gels and creams
- Its primary commercial use is in products targeting severe recalcitrant nodular acne
- The API is approved and marketed in the US and Canada
Clinical Overview
Isotretinoin is a vitamin A derivative within the retinoid class. Its pharmacodynamic profile is not fully elucidated, but clinical activity is attributed to coordinated effects on cell cycle progression, differentiation, sebocyte survival, and apoptosis. These actions lead to marked suppression of sebum production, reduction of ductal obstruction, and decreased formation of comedones. Isotretinoin itself has minimal affinity for retinol binding proteins or retinoic acid receptors. Metabolites such as 4‑oxo‑isotretinoin and retinoic acid derivatives demonstrate receptor interactions, including activity at RAR‑γ. Additional mechanisms may involve modulation of immune responses, altered monocyte chemotaxis, and potential interaction with the transcription factor FoxO1.
Isotretinoin does not possess direct antibacterial activity, but by reducing sebum output and altering follicular conditions, it creates an environment less supportive of Cutibacterium acnes proliferation.
Following oral administration, absorption is variable and increases significantly when taken with dietary fat. The compound undergoes extensive hepatic metabolism, including pathways associated with CYP3A. Circulating metabolites contribute to overall pharmacologic effect. Elimination occurs through both renal and biliary routes. Isotretinoin is highly lipophilic and extensively protein bound.
Safety considerations are dominated by its well‑established teratogenicity. Strict pregnancy prevention measures and controlled distribution programs are required in several regulatory jurisdictions. Additional concerns include potential hepatotoxicity, dyslipidemia, mucocutaneous effects, and photosensitivity.
For API procurement, sourcing should prioritize validated manufacturers with retinoid‑appropriate handling controls, demonstrated impurity management, and compliance with regional retinoid risk‑mitigation requirements to support consistent quality and regulatory acceptance.
Identification & chemistry
| Generic name | Isotretinoin |
|---|---|
| Molecule type | Small molecule |
| CAS | 4759-48-2 |
| UNII | EH28UP18IF |
| DrugBank ID | DB00982 |
Pharmacology
| Summary | Isotretinoin modulates cell differentiation, proliferation, and apoptosis in sebocytes, leading to substantial reductions in sebum production and comedone formation. Its activity is mediated largely through metabolites that interact with retinoic acid receptors, particularly RAR‑γ, with additional effects on keratinization, inflammation, and the follicular microenvironment. The drug’s overall pharmacodynamic profile remains only partially defined, with emerging evidence implicating pathways such as FoxO1 signaling. |
|---|---|
| Mechanism of action | Isotretinoin produces its effects through altering progress through the cell cycle, cell differentiation, survival, and apoptosis.These actions reduce sebum production, preventing the blockage of pores, and growth of acne causing bacteria.Isotretinoin and 4-oxo-isotretinoin both significantly reduce the production of sebum.[A179091,Label] Isotretinoin has little to no affinity for retinol binding proteins (RBPs) and retinoic acid nuclear receptors (RARs).Tretinoin and 4-oxo-tretinion bind to the RAR-γ receptor, which is suspected to be part of the action of acne treatment by isotretinoin.Isotretinoin induces apoptosis in sebocytes, leading to a decrease in sebum production.Isotretinoin also reduces the formation of comedones by reducing hyperkeratinization through an unknown mechanism.Isotretinoin does not directly kill bacteria but it does reduce the size of sebum ducts and makes the microenvironment less hospitable to acne causing bacteria.It may also increase immune mechanisms and alter chemotaxis of monocytes to reduce inflammation. There is preliminary evidence suggesting isotretinoin may interact with FoxO1, which may explain a substantial number of isotretinoin's unexplained actions. |
| Pharmacodynamics | The pharmacodynamics of isotretinoin are poorly understood.[Label] |
Targets
| Target | Organism | Actions |
|---|---|---|
| Retinoic acid receptor gamma | Humans | |
| Retinoic acid receptor alpha | Humans | other/unknown |
ADME / PK
| Absorption | Patients reach a maximum concentration of 74-511ng/mL after 1-4 hours following a 100mg oral dose.Isotretinoin is better absorbed with a high fat meal and bioavailability may change from one brand to another.[Label] Following a 40mg oral dose, fasted subjects reached a maximum concentration of 314ng/mL in 2.9 hours with an area under the curve of 4055ng/mL\*hr.[Label] Subjects given a high fat meal and a 40mg oral doses reached a maximum concentration of 395ng/mL in 6.4 hours with an area under the curve of 6095ng/mL\*mL.[Label] |
|---|---|
| Half-life | The half life ranges from 7-39 hourswith a mean elimination half life of 20 hours.The half life of 4-oxo-13-cis-retinoic acid ranges from 17-50 hours with a mean elimination half life of 25 hours. |
| Protein binding | Isotretinoin is >99.9% protein bound, mainly to serum albumin.[Label] |
| Metabolism | Isotretinoin, or 13-cis-retinoic acid can undergo reversible cis-trans isomerization to all-trans-retinoic acid.Isotretinoin undergoes 4-hydroxylation to 4-hydroxy-13-cis-retinoic acid, which is oxidized to the main metabolite 4-oxo-13-cis-retinoic acid.. All-trans-retinoic acid undergoes 4-hydroxylation to 4-hydroxy-all-trans-retinoic acid, which is oxidized to 4-oxo-all-trans-retinoic acid.4-oxo-13-cis-retinoic acid can undergo reversible cis-trans isomerization to 4-oxo-all-trans-retinoic acid. |
| Route of elimination | Isotretinoin and its metabolites are conjugated and excreted in the urine and feces in similar amounts.[Label] 53-74% of an oral dose is eliminated as unchanged isotretinoin in the feces. |
| Volume of distribution | The volume of distribution in humans is unknown because there is no intravenous preparation.In a study of pediatric patients with neuroblastoma the volume of distribution was found to be 85L.The volume of distribution was also found to be 2432mL/kg in guinea pigs and 1716mL/kg in obese rats. |
| Clearance | The clearance of isotretinoin is 15.9L/h in pediatric patients with neuroblastoma.Clearance is also 21.3mL/min/kg in guinea pigs and 7.2mL/min/kg in obese rats. |
Formulation & handling
- Oral formulations require lipid-containing excipients or delivery systems to overcome very low aqueous solubility and support absorption, which is enhanced when taken with high‑fat meals.
- The photosensitive, oxidation‑prone retinoid structure necessitates protection from light and oxygen during manufacturing and storage.
- Topical products use gels or creams to stabilize the lipophilic API and require formulation strategies that minimize degradation while controlling skin penetration.
Regulatory status
| Lifecycle | With all listed U.S. patents expiring in 2021 and the product marketed in the US and Canada, the API is in a post‑exclusivity phase. Market conditions are consistent with a mature segment where generic competition is established. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Isotretinoin’s supply chain includes multiple manufacturers and repackagers, with the originator’s role now largely limited to branded references while numerous generic-capable firms participate in production and distribution. Branded products are established primarily in the US and Canadian markets. With key US patents expiring in 2021, the molecule is already subject to broad generic competition. |
|---|
Safety
| Toxicity | Patients experiencing an overdose may present with vomiting, facial flushing, cheilosis, abdominal pain, headache, dizziness, and ataxia.[Label] These symptoms may rapidly resolve.[Label] Generally no treatment is required for these overdoses. The oral lowest dose causing toxic effect (TDLO) for children is 30mg/kg/21W, oral TDLO for men is 24mg/kg/4W, oral TDLO for women is 56mg/kg/8W.The intraperitoneal LD<sub>50</sub> for rats is 901mg/kg, oral LD<sub>50</sub> for mice is 3389mg/kg, oral LD<sub>50</sub> for rats is >4000mg/kg. Isotretinoin is associated with major congenital malformations, spontaneous abortion, and premature birth.[Label] It is unknown if isotretinoin is expressed in breast milk but due to the associated hazards a decision should be made to either stop nursing or stop taking isotretinoin.[Label] In animal studies, isotretinoin was associated with an increased risk of pheochromocytoma and adrenal medullary hyperplasia at doses above the recommended clinical dose.[Label] Isotretinoin was negative for the Ames test of mutagenicity once and weakly positive a second time.[Label] It has not been shown to be clastogenic.[Label] A study in dogs noted testicular atrophy after doses of 10-30 times the recommended clinical dose for 30 weeks.[Label] In trials with men there were no effects seen on sperm count, motility, morphology, ejaculate volume, and seminal plasma fructose.[Label] |
|---|
- Exhibits dose‑dependent systemic toxicity
- Documented TDLO ranges from 24–56 mg/kg (humans) and acute LD50 values exceed 900 mg/kg intraperitoneal (rat) and 3000 mg/kg orally (mouse), indicating relatively low acute lethality but measurable subchronic toxicity at elevated exposures
- Teratogenic hazards are significant, with documented major congenital malformations and pregnancy‑related adverse outcomes
Isotretinoin is a type of Dermatics
Dermatics is a prominent subcategory within the pharmaceutical Active Pharmaceutical Ingredient (API) sector. It focuses on the development and production of APIs specifically designed for dermatological applications. These APIs play a crucial role in the formulation of various pharmaceutical products used in the treatment of skin disorders, including creams, ointments, gels, and lotions.
Dermatics APIs are meticulously developed to address specific dermatological conditions such as acne, psoriasis, eczema, fungal infections, and other related ailments. The APIs used in these formulations are carefully selected for their therapeutic efficacy, safety, and compatibility with the skin.
Manufacturers of Dermatics APIs employ rigorous quality control measures to ensure the purity, potency, and stability of their products. These APIs undergo extensive testing to meet stringent regulatory standards and pharmacopoeial guidelines. Additionally, the production processes adhere to Good Manufacturing Practices (GMP) to guarantee consistent quality and minimize the risk of contamination.
With the increasing demand for advanced dermatological treatments, Dermatics APIs are subject to continuous research and development. Newer APIs are being explored to enhance efficacy, minimize side effects, and improve patient compliance. The field of Dermatics APIs is characterized by innovation, as researchers strive to develop novel compounds and delivery systems that address unmet therapeutic needs.
In summary, Dermatics APIs are a vital component of pharmaceutical formulations used in the treatment of skin disorders. They undergo stringent quality control measures and are constantly evolving to provide effective and safe dermatological solutions.
Isotretinoin (Dermatics), classified under Dermatological Agents
Dermatological agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the formulation of various skincare and dermatology products. These APIs are specifically designed to target and treat skin conditions, offering effective solutions for a wide range of dermatological concerns.
Dermatological agents encompass a diverse array of compounds, including corticosteroids, antifungal agents, antibacterials, retinoids, and immunomodulators. Each API within this category possesses unique properties and mechanisms of action, enabling them to address specific skin-related issues.
Corticosteroids, for instance, are potent anti-inflammatory agents commonly used in the treatment of skin conditions like eczema, psoriasis, and dermatitis. Antifungal agents, on the other hand, combat fungal infections such as athlete's foot or ringworm. Antibacterials are effective against bacterial infections, while retinoids promote skin cell turnover and treat acne and photoaging. Immunomodulators regulate the immune response, providing relief from conditions like atopic dermatitis.
The development and application of dermatological APIs involve rigorous research, clinical trials, and regulatory compliance. These APIs are typically integrated into topical creams, ointments, gels, and lotions, ensuring targeted delivery to the affected areas of the skin.
Dermatological agents play a crucial role in the management and treatment of various skin disorders. By harnessing the therapeutic properties of these APIs, pharmaceutical companies can develop innovative skincare products that cater to the diverse needs of individuals seeking effective dermatological solutions.
Isotretinoin API manufacturers & distributors
Compare qualified Isotretinoin API suppliers worldwide. We currently have 9 companies offering Isotretinoin 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 |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CoA, USDMF | 46 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA, GMP | 70 products |
| F Hoffmann-La Roche | Producer | Switzerland | Switzerland | CEP, CoA, FDA | 8 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Shanghai New Hualian | Producer | China | China | CEP, CoA, WC | 2 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Socosur | Distributor | France | Unknown | CoA | 21 products |
| Sun Pharma | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 219 products |
When sending a request, specify which Isotretinoin 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 Isotretinoin 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 Isotretinoin API
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Technical
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Regulatory
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