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Pentostatin | CAS No: 53910-25-1 | GMP-certified suppliers
A medication that treats hairy cell leukemia refractory to alpha interferon by targeting malignant lymphoid cells with antineoplastic and immunosuppressive effects.
Therapeutic categories
Primary indications
- For the treatment of hairy cell leukaemia refractory to alpha interferon
Product Snapshot
- Pentostatin is available as oral coated tablets and injectable lyophilized powder formulations
- It is indicated primarily for the treatment of refractory hairy cell leukemia
- Pentostatin is approved or investigational in key markets including the US and Canada
Clinical Overview
Clinically, pentostatin is approved for the treatment of hairy cell leukemia refractory to alpha interferon. It exerts antineoplastic effects by acting as a purine analog, specifically a 6-thiopurine analogue structurally related to naturally occurring purine bases hypoxanthine and guanine. Intracellularly, it undergoes activation leading to incorporation into DNA and RNA as a false purine base. This incorporation disrupts nucleic acid synthesis during the S phase of the cell cycle, thereby inhibiting cell replication selectively in malignant lymphoid cells. Additionally, ADA inhibition results in accumulation of intracellular deoxyadenosine nucleotides such as dATP, which further impairs DNA synthesis via ribonucleotide reductase inhibition, contributing to its cytotoxic effect.
Pharmacodynamically, pentostatin exhibits cell cycle phase specificity targeting the DNA synthesis phase, and exerts synergistic effects with other antineoplastic agents. It also possesses immunosuppressive properties related to its interference with lymphocyte proliferation.
Regarding absorption, distribution, metabolism, and excretion (ADME), pentostatin is predominantly eliminated by renal excretion, necessitating attention to renal function during treatment. The drug has a narrow therapeutic index, highlighting the need for careful dose management and monitoring.
Safety considerations include potential myelosuppression, immunosuppression, and cardiotoxicity. These toxicities require vigilant clinical assessment during therapy. Pentostatin’s use is generally confined to specialist oncology and hematology settings due to these safety concerns.
Notable therapeutic contexts include its role in combination chemotherapy regimens for hairy cell leukemia and certain other lymphoproliferative malignancies. While investigational uses continue to be explored, current approvals focus on refractory hairy cell leukemia.
From a sourcing perspective, procuring pentostatin APIs demands strict adherence to quality standards, including validation of chemical purity, control of residual solvents, and confirmation of identity due to its complex synthetic pathway and narrow therapeutic window. Suppliers must comply with Good Manufacturing Practice (GMP) regulations to ensure consistent supply suitable for clinical-grade formulations.
Identification & chemistry
| Generic name | Pentostatin |
|---|---|
| Molecule type | Small molecule |
| CAS | 53910-25-1 |
| UNII | 395575MZO7 |
| DrugBank ID | DB00552 |
Pharmacology
| Summary | Pentostatin is a purine analog that acts as a potent inhibitor of adenosine deaminase, primarily affecting lymphoid cells with high enzymatic activity. Its mechanism involves the accumulation of toxic metabolites that inhibit DNA synthesis by blocking ribonucleotide reductase, leading to cell cycle-specific cytotoxicity during the S-phase. Pentostatin is utilized for its antineoplastic effects, particularly in the treatment of certain leukemias refractory to other therapies. |
|---|---|
| Mechanism of action | Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. T-cells have higher ADA activity than B-cells, and T-cell malignancies have higher activity than B-cell malignancies. The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated intracellular levels of dATP, which can block DNA synthesis through inhibition of ribonucleotide reductase. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase). |
| Pharmacodynamics | Pentostatin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Adenosine deaminase | Humans | inhibitor |
ADME / PK
| Absorption | Not absorbed orally, crosses blood brain barrier. |
|---|---|
| Half-life | 5.7 hours (with a range between 2.6 and 16 hrs) |
| Protein binding | 4% |
| Metabolism | Primarily hepatic, but only small amounts are metabolized. |
| Route of elimination | In man, following a single dose of 4 mg/m2 of pentostatin infused over 5 minutes, approximately 90% of the dose was excreted in the urine as unchanged pentostatin and/or metabolites as measured by adenosine deaminase inhibitory activity. |
| Clearance | * 68 mL/min/m2 |
Formulation & handling
- Pentostatin is formulated for both oral administration as coated tablets and intravenous use as lyophilized powder requiring reconstitution.
- The compound's high water solubility and low logP indicate favorable aqueous formulation properties but necessitate protection from moisture during storage.
- Handling should consider stability of lyophilized injectable forms, with appropriate reconstitution protocols to maintain potency.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, allowing for generic entry and increased market competition. As a result, the product is in a mature phase with established presence across these markets. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Pentostatin is manufactured by multiple originator companies, including Hospira Inc. and Bedford Laboratories, with several packagers involved in the supply chain. Its branded products are primarily distributed in the US and Canadian markets. Patent expiries indicate the presence of existing generic competition in these regions. |
|---|
Safety
| Toxicity | LD<sub>50</sub>=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression. |
|---|
- Handle with appropriate personal protective equipment to avoid dermal and inhalation exposure due to potential systemic toxicity
- Use in well-ventilated areas to minimize inhalation risk, given observed adverse effects including myelosuppression
- Avoid skin contact
Pentostatin is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
Pentostatin API manufacturers & distributors
Compare qualified Pentostatin API suppliers worldwide. We currently have 2 companies offering Pentostatin API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| ChemPacific | Producer | United States | Unknown | CoA, USDMF | 10 products |
| Hospira Boulder | Producer | United States | United States | CoA, JDMF | 5 products |
When sending a request, specify which Pentostatin 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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