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Didanosine | CAS No: 69655-05-6 | GMP-certified suppliers
A medication that, in combination with other antiretrovirals, is used for treating HIV-1 infection in adults by enhancing virologic suppression and interrupting viral replication.
Therapeutic categories
Primary indications
- For use, in combination with other antiretroviral agents, in the treatment of HIV-1 infection in adults
Product Snapshot
- Didanosine is available primarily as oral small molecule formulations, including extended-release capsules, chewable tablets, delayed-release capsules, and powders for solution
- It is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults
- Didanosine is approved for use in key regulatory markets, including the United States and Canada
Clinical Overview
Pharmacologically, didanosine is a nucleoside reverse transcriptase inhibitor (NRTI). Structurally, it differs from other nucleoside analogues by the presence of a hypoxanthine base linked to a sugar moiety lacking hydroxyl groups at the 2' and 3' positions. This modification impairs the ability to form phosphodiester bonds critical for nucleic acid chain elongation. Upon cellular uptake, didanosine undergoes phosphorylation by host enzymes to its active metabolite, dideoxyadenosine triphosphate (ddATP).
The active metabolite competitively inhibits HIV reverse transcriptase by mimicking the natural substrate deoxyadenosine triphosphate (dATP). Once incorporated into viral DNA, ddATP acts as a chain terminator due to the absent 3’-hydroxyl group, preventing further elongation of the viral DNA strand and thereby interrupting HIV replication. This mechanism underscores its antiviral effect in systemic HIV treatment regimens.
Key absorption and metabolic considerations include didanosine’s weak acid stability, often necessitating co-administration with antacids to mitigate degradation in gastric acid conditions. Following absorption, the drug is distributed intracellularly where activation occurs. Didanosine is primarily cleared via renal elimination, highlighting the need for dose adjustment in patients with renal impairment.
Safety considerations include potential adverse reactions associated with mitochondrial toxicity, such as peripheral neuropathy and pancreatitis. Neurotoxic effects have been documented, requiring careful clinical monitoring. Didanosine is classified as an enzyme inhibitor and has interactions relevant to other antiretrovirals and concomitant medications.
Several branded formulations of didanosine have been marketed globally; however, its use has declined with the availability of newer agents with improved safety profiles.
From an API sourcing and quality perspective, it is essential to ensure didanosine raw material complies with pharmacopeial standards regarding purity, residual solvents, and impurity profiles. Stability under weakly acidic and alkaline conditions should be confirmed to maintain potency. Additionally, due to its sensitivity to degradation, appropriate handling and storage conditions must be observed throughout manufacturing and supply chain processes.
Identification & chemistry
| Generic name | Didanosine |
|---|---|
| Molecule type | Small molecule |
| CAS | 69655-05-6 |
| UNII | K3GDH6OH08 |
| DrugBank ID | DB00900 |
Pharmacology
| Summary | Didanosine is a nucleoside reverse transcriptase inhibitor that targets the HIV-1 reverse transcriptase enzyme. Intracellularly phosphorylated to its active form, it competitively inhibits reverse transcriptase and terminates viral DNA chain elongation by incorporation into the viral genome. This mechanism disrupts viral replication, supporting its use in combination antiretroviral therapy for HIV-1 infection. |
|---|---|
| Mechanism of action | Didanosine (ddI) is metabolized intracellularly by a series of cellular enzymes to its active moiety, dideoxyadenosine triphosphate (ddATP), which inhibits the HIV reverse transcriptase enzyme competitively by competing with natural dATP. It also acts as a chain terminator by its incorporation into viral DNA as the lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. |
| Pharmacodynamics | Didanosine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Didanosine is a hypoxanthine attached to the sugar ring, unlike other nucleoside analogues. Didanosine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. Didanosine is effective against HIV, and usually used in combination with other antiviral therapy. Switching from long term AZT treatment to didanosine has been shown to be beneficial. Didanosine has weak acid stability and therefore, it is often combined with an antacid. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | inhibitor |
| Purine nucleoside phosphorylase | Humans | substrate |
ADME / PK
| Absorption | Rapidly absorbed (bioavailability 30-40%) with peak plasma concentrations appearing within 0.5 and 1.5 hrs. |
|---|---|
| Half-life | 30 minutes in plasma and more than 12 hours in intracellular environment. |
| Protein binding | Low (<5%) |
| Metabolism | Rapidly metabolized intracellularly to its active moiety, 2,3-dideoxyadenosine-5-triphosphate (ddA-TP). It is then further metabolized hepatically to yield hypoxanthine, xanthine, and uric acid. |
| Route of elimination | Based on data from in vitro and animal studies, it is presumed that the metabolism of didanosine in man occurs by the same pathways responsible for the elimination of endogenous purines. Purines are eliminated by the kidneys. |
Formulation & handling
- Didanosine is a small molecule antiviral primarily formulated for oral administration, including extended and delayed release capsules, chewable, and suspension tablets.
- It requires administration on an empty stomach, with at least a one-hour gap before or two hours after meals to optimize absorption and reduce food interaction effects.
- Handling should consider its moderate aqueous solubility and solid state stability, avoiding exposure to moisture and alcohol which may affect product performance.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's patent protection has expired in both the United States (2012) and Canada (2011 and 2018), indicating that the product is currently in a mature market phase with potential availability of generic versions in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Didanosine is manufactured by multiple originator and generic companies, including Bristol Myers Squibb as the originator and several generic manufacturers such as Aurobindo Pharma and Barr Laboratories. Its branded products are primarily present in the US and Canadian markets. Patent expirations between 2011 and 2018 indicate that generic competition is established in these regions. |
|---|
Safety
| Toxicity | Side effects include pancreatitis, peripheral neuropathy, diarrhea, hyperuricemia and hepatic dysfunction |
|---|
- 1
- May cause hepatotoxicity
- Monitor liver function during manufacture and handling
Didanosine is a type of Anti-HIV
The Anti-HIV category of pharmaceutical APIs comprises a range of active pharmaceutical ingredients (APIs) specifically designed to combat the human immunodeficiency virus (HIV). These APIs play a critical role in the development and production of antiretroviral drugs, which are used to treat HIV infections and prevent the progression to acquired immunodeficiency syndrome (AIDS).
Anti-HIV APIs work by targeting various stages of the HIV life cycle, inhibiting viral replication and reducing the viral load in the body. Some commonly used APIs in this category include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), and integrase inhibitors (INIs).
NRTIs, such as tenofovir and emtricitabine, act by blocking the reverse transcriptase enzyme, an essential component in the replication of the virus. NNRTIs, such as efavirenz and nevirapine, bind to the reverse transcriptase enzyme, preventing its proper functioning. PIs, like ritonavir and atazanavir, inhibit the protease enzyme, crucial for viral maturation and assembly. INIs, such as raltegravir and dolutegravir, target the integrase enzyme, impeding viral integration into the host's DNA.
These APIs are carefully synthesized and undergo rigorous quality testing to ensure their safety, efficacy, and compliance with regulatory standards. Pharmaceutical companies utilize these APIs as key building blocks to formulate antiretroviral medications, which are then prescribed to individuals living with HIV/AIDS worldwide.
Overall, the Anti-HIV API category plays a vital role in the ongoing battle against HIV/AIDS, offering effective treatment options and improved quality of life for patients affected by this challenging condition.
Didanosine API manufacturers & distributors
Compare qualified Didanosine API suppliers worldwide. We currently have 3 companies offering Didanosine API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Hetero Labs | Producer | India | India | CoA, GMP, WC | 90 products |
| Mylan | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF | 201 products |
| Shandong Zhanhua Yonghao | Producer | China | China | CoA | 10 products |
When sending a request, specify which Didanosine 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 Didanosine 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.
