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Zalcitabine | CAS No: 7481-89-2 | GMP-certified suppliers
A medication that treats HIV infections by inhibiting viral replication when used with other antivirals, requiring careful quality control for purity and safety in API sourcing.
Therapeutic categories
Primary indications
- For the treatment of Human immunovirus (HIV) infections in conjunction with other antivirals
Product Snapshot
- Zalcitabine is an oral small molecule formulated primarily as film-coated tablets
- It is indicated for use in combination antiviral therapy for HIV infections
- The product is approved and marketed in the US and Canada
Clinical Overview
Pharmacologically, zalcitabine acts as a nucleoside reverse transcriptase inhibitor (NRTI). It is an analog of 2'-deoxycytidine but differs structurally from other NRTIs. Upon intracellular uptake, zalcitabine is phosphorylated sequentially by cellular kinases to its active triphosphate form, dideoxycytidine 5'-triphosphate (ddCTP). The active metabolite competes with the natural substrate, deoxycytidine 5'-triphosphate (dCTP), for incorporation by the viral reverse transcriptase enzyme during viral DNA synthesis.
The unique mechanism of action arises from the absence of the 3' hydroxyl group on zalcitabine's sugar moiety, which is required for forming 5' to 3' phosphodiester bonds during DNA elongation. Incorporation of ddCTP into the viral DNA strand results in premature chain termination, effectively inhibiting the replication of HIV-1.
Pharmacokinetic data including absorption, distribution, metabolism, and excretion parameters are variable based on formulation and patient population, with intracellular phosphorylation being critical for activity.
Safety considerations are notable due to the principal toxic effect of axonal degeneration, which can lead to peripheral neuropathy. This neurotoxicity requires careful monitoring during therapy. Other adverse effects should be evaluated in the context of combination antiretroviral treatment regimens.
Zalcitabine has been approved in various regulatory contexts as part of antiretroviral therapy, although it is less commonly used in contemporary practice due to safety profiles and the availability of newer agents.
For API sourcing, quality control should emphasize purity, stereochemical integrity, and the absence of degradation products or contaminants. Compliance with pharmacopeial standards and regulatory guidelines is essential to ensure consistent potency and safety of the active pharmaceutical ingredient.
Identification & chemistry
| Generic name | Zalcitabine |
|---|---|
| Molecule type | Small molecule |
| CAS | 7481-89-2 |
| UNII | 6L3XT8CB3I |
| DrugBank ID | DB00943 |
Pharmacology
| Summary | Zalcitabine is a nucleoside reverse transcriptase inhibitor (NRTI) targeting HIV-1 by inhibiting viral reverse transcriptase activity. It is intracellularly converted to dideoxycytidine triphosphate, which competes with natural nucleotides and incorporates into viral DNA, causing premature chain termination. This mechanism disrupts viral DNA synthesis and replication, contributing to antiretroviral therapy. |
|---|---|
| Mechanism of action | Zalcitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Within cells, zalcitabine is converted to its active metabolite, dideoxycytidine 5'-triphosphate (ddCTP), by the sequential action of cellular enzymes. ddCTP interferes with viral RNA-directed DNA polymerase (reverse transcriptase) by competing for utilization of the natural substrate deoxycytidine 5'-triphosphate (dCTP), as well as incorpating into viral DNA. Due to it's lack of a 3'-OH group, the formation of a 5' to 3' phosphodiester linkage that is necessary for DNA chain elongation is inhibited, thus leading to the termination of viral DNA growth. |
| Pharmacodynamics | Zalcitabine is an analog of 2'-deoxycytidine that is pharmacologically related to but structurally different from other nucleotide reverse transcriptase inhibitors (NRTIs). Zalcitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | Bioavailability is over 80% following oral administration. |
|---|---|
| Half-life | 2 hours |
| Protein binding | Less than 4% |
| Metabolism | Zalcitabine is not reported to undergo significant hepatic metabolism; it is mainly phosphorylated intracellularly to zalcitabine triphosphate, the active substrate for HIV-reverse transcriptase. The concentration of zalcitabine triphosphate remains low for quantitative detection and measurement in the plasma following administration of therapeutic doses. |
| Route of elimination | Renal excretion of unchanged drug appears to be the primary route of elimination, accounting for approximately 80% of an intravenous dose and 60% of an orally administered dose within 24 hours after dosing (n=19). Renal clearance exceeds glomerular filtration rate suggesting renal tubular secretion contributes to the elimination of zalcitabine by the kidneys. |
| Volume of distribution | * 0.304 to 0.734 L/kg |
| Clearance | * 285 mL/min [HIV-infected patients receiving 1.5 mg IV infusion for 1 hour] |
Formulation & handling
- Zalcitabine is a small molecule nucleoside analogue formulated exclusively for oral administration in tablet form.
- This API exhibits sensitivity to multivalent ions; co-administration with magnesium or aluminum-containing compounds may impair absorption.
- Optimal bioavailability is achieved when taken on an empty stomach, at least 1 hour before or 2 hours after meals.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has reached patent expiry in both the US and Canadian markets, indicating entry into the mature phase of its lifecycle with the presence of generic equivalents. Market availability is well established across these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Zalcitabine is currently manufactured by a single originator company, Hoffmann-La Roche Inc., with branded products marketed primarily in the US and Canadian markets. The presence of multiple brand formulations indicates established branded product availability in these regions. Given the lack of multiple manufacturers and limited geographic distribution, patent expiry may allow for potential generic competition, though current supply remains focused on the originator’s branded products. |
|---|
Safety
| Toxicity | Acute overdose: Inadvertent pediatric overdoses have occurred with doses up to 1.5 mg/kg zalcitabine. Chronic overdose: in an initial dose-finding study in which zalcitabine was administered at doses 25 times (0.25 mg/kg every 8 hours) the currently recommended dose, one patient discontinued zalcitabine after 1½ weeks of treatment subsequent to the development of a rash and fever. |
|---|
- Handling zalcitabine requires precautions to minimize exposure due to potential toxicity observed in acute and chronic overdose scenarios
- Avoid inadvertent pediatric exposure
- Doses as low as 1
Zalcitabine 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.
Zalcitabine API manufacturers & distributors
Compare qualified Zalcitabine API suppliers worldwide. We currently have 2 companies offering Zalcitabine API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Hangzhou Jinlan Pharm-Dru... | Producer | China | China | CEP, CoA, GMP | 40 products |
| Shandong Zhanhua Yonghao | Producer | China | China | CoA | 10 products |
When sending a request, specify which Zalcitabine 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.).
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