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Nedaplatin | CAS No: 95734-82-0 | GMP-certified suppliers
A medication that treats various cancers including non-small cell lung, small cell lung, esophageal, and head and neck cancers with effective antitumor activity and reduced nephrotoxicity.
Therapeutic categories
Primary indications
- Used in the treatment of non-small cell lung cancer, small cell lung cancer, oesophygeal cancer, and head and neck cancers
Product Snapshot
- Nedaplatin is an injectable small molecule platinum-based chemotherapy agent
- It is primarily indicated for the treatment of non-small cell lung cancer, small cell lung cancer, esophageal cancer, and head and neck cancers
- The compound holds both approved and investigational regulatory statuses in various markets
Clinical Overview
Pharmacodynamically, nedaplatin acts by inducing DNA damage that triggers cancer cell death. Its mechanism is comparable to other platinum analogs. After cellular uptake, nedaplatin undergoes hydrolysis to form an active species that complexes with intracellular water molecules. This active form binds to nucleophilic sites such as glutathione and cysteine-rich proteins, disrupting the cell’s antioxidant capacity and generating oxidative stress. It also interacts with purine nucleotides in DNA, forming intra- and interstrand cross-links predominantly at guanine residues.
These cross-links hinder DNA replication and transcription and are recognized by DNA repair proteins, including high mobility group proteins and the mismatch repair (MMR) complex. The MMR complex attempts to excise the damage but its repair efforts create single-strand breaks which eventually lead to double-strand breaks, activating apoptosis pathways. This mechanism underlies both its cytotoxicity and its radiosensitizing properties, where nedaplatin enhances cancer cell susceptibility to radiation therapy.
Nedaplatin exhibits lower nephrotoxicity relative to cisplatin, a widely used first-generation platinum compound, while maintaining comparable antitumor efficacy. It is primarily excreted renally and is categorized as a narrow therapeutic index drug, necessitating careful dosing and monitoring for toxicity, particularly renal function. Other safety considerations include potential myelosuppression and gastrointestinal adverse effects consistent with platinum-based agents.
For API sourcing, quality considerations include stringent control of residual solvents and heavy metal impurities, as well as verifying the compound’s physicochemical purity and stability. Regulatory compliance with international pharmacopeial standards and Good Manufacturing Practice (GMP) is essential to ensure product consistency and safety in clinical applications.
Identification & chemistry
| Generic name | Nedaplatin |
|---|---|
| Molecule type | Small molecule |
| CAS | 95734-82-0 |
| UNII | 8UQ3W6JXAN |
| DrugBank ID | DB13145 |
Pharmacology
| Summary | Nedaplatin is a platinum-based chemotherapeutic agent that exerts cytotoxic effects by forming DNA cross-links, leading to apoptosis through interference with DNA replication and repair. It binds to glutathione and other cysteine-rich proteins, increasing oxidative stress within the cell. Nedaplatin also acts as a radiosensitizer by enhancing the formation of lethal DNA double-strand breaks in response to radiation therapy. |
|---|---|
| Mechanism of action | As a platinum analog, nedaplatin likely works similarly to [DB00515] on which the following mechanistic description is based. Once it has entered the cell it is hydrolyzed to its active form which complexes with water molecules . This form binds to to nucleophiles in the cytoplasm such as glutathione and other cyteine rich proteins resulting in an overall increase in oxidative stress as the cell loses antioxidant proteins. It also binds to purine nucleotides in the DNA. The active form allows for two binding interactions to form cross-links between these nucleotides. High mobility group proteins-1 and -2 induce apoptosis in response to guanine cross-links and their binding serves to shield the cross-linked DNA from repair mechanisms. The mismatch repair (MMR) protein complex also recognizes the distortion caused by platinum complexes and attempts to repair the DNA. This results in single strand breaks when the MMR complex attempts to remove the platinum cross-link. The MMR complex induces apoptosis after the repair attempt has failed. The single strand break in DNA makes it easier to form lethal double strand breaks with radiation treatment thus creating the radiosensitizing effect of nedaplatin . |
| Pharmacodynamics | Nedaplatin damages DNA and induces cell death in cancer cells . It also functions as a radiosensitizer, increasing the susceptibility of the affected cells to radiation therapy . |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | ligand |
| Glutathione | Humans | ligand |
ADME / PK
| Protein binding | Approximately 50% of the platinum from nedaplatin appears to be bound to human plasma proteins . |
|---|---|
| Route of elimination | Most of the platinum from nedaplatin is eliminated in the urine (59.6%) . |
| Volume of distribution | The volume of distribution of free platinum is 12.0 L . |
| Clearance | Clearance of the free platinum is 4.47 L/h . |
Formulation & handling
- Nedaplatin is a small molecule with high water solubility suitable for injectable formulations.
- Its low LogP value indicates limited membrane permeability, relevant for bioavailability considerations.
- As a carboxylic acid salt in solid form, Nedaplatin requires careful handling to maintain stability and prevent moisture uptake.
Regulatory status
Safety
| Toxicity | The toxic effects of nedaplatin are likely similar to those of [DB00515] which produces nausea, vomiting, peripheral neuropathy, and ototoxicity . A major difference between the compounds is the large reduction in nephrotoxicity of nedaplatin compared to [DB00515] . |
|---|
- Nedaplatin exhibits lower nephrotoxicity relative to similar platinum-based compounds
- Exposure may result in adverse effects such as nausea, vomiting, peripheral neuropathy, and ototoxicity
- Appropriate handling measures should be employed to minimize risk of systemic toxicity
Nedaplatin 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.
Nedaplatin API manufacturers & distributors
Compare qualified Nedaplatin API suppliers worldwide. We currently have 1 companies offering Nedaplatin 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 |
|---|---|---|---|---|---|
| Shandong Boyuan | Producer | China | China | CoA | 55 products |
When sending a request, specify which Nedaplatin 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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