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Telaprevir | CAS No: 402957-28-2 | GMP-certified suppliers
A medication that inhibits NS3/4A protease for treating chronic hepatitis C virus genotype 1 infection, used in combination to improve sustained virologic response in adult patients.
Therapeutic categories
Primary indications
- Telaprevir, when used in combination with [DB00811], [DB00008], and [DB00022] is indicated for use in the treatment of chronic HCV genotype 1 infection in adults
Product Snapshot
- Telaprevir is an oral small molecule formulated as film-coated tablets
- It is indicated for combination therapy in the treatment of chronic hepatitis C virus genotype 1 infection in adults
- Telaprevir has received regulatory approval in the US, Canada, and the EU but has been withdrawn in certain markets
Clinical Overview
The primary mechanism of action of Telaprevir involves potent and selective inhibition of the NS3/4A protease, with an IC50 of approximately 10 nM, thereby disrupting viral replication. This class of protease inhibitors exhibits a lower barrier to resistance compared to NS5B polymerase inhibitors. Resistance-associated substitutions at amino acid positions 155, 156, or 168 within NS3/4A reduce drug binding affinity and compromise efficacy. Mutations affecting the enzyme’s catalytic triad (H58, D82, S139) also impact Telaprevir’s inhibitory activity.
Pharmacokinetic data indicate that Telaprevir is a substrate and strong inhibitor of cytochrome P450 CYP3A4, and also interacts with drug transporters such as OATP1B1 and P-glycoprotein, influencing its absorption and disposition profile. Drug-drug interactions are thus a key consideration in clinical use.
Safety and toxicity profiles include typical antiviral adverse reactions and considerations related to CYP3A-mediated interactions. Clinical use of Telaprevir was as part of combination regimens including pegylated interferon and ribavirin to achieve sustained virologic response (SVR), defined as undetectable HCV RNA 12 weeks post-therapy. SVR is associated with long-term benefits such as reduced hepatic fibrosis progression and hepatocellular carcinoma incidence.
Telaprevir was marketed under the trade name Incivek following FDA approval in 2011 but has since been withdrawn from the market due to the availability of newer agents with improved efficacy and safety profiles. For API procurement, strict adherence to quality standards concerning purity, polymorphic form, and residual solvents is essential. Given its complex peptide-based structure and sensitivity to enzymatic degradation, sourcing from manufacturers with validated synthetic routes and robust quality control measures is recommended to ensure consistency and compliance with regulatory expectations.
Identification & chemistry
| Generic name | Telaprevir |
|---|---|
| Molecule type | Small molecule |
| CAS | 402957-28-2 |
| UNII | 655M5O3W0U |
| DrugBank ID | DB05521 |
Pharmacology
| Summary | Telaprevir is a direct-acting antiviral agent that targets the NS3/4A serine protease, a key enzyme required for cleavage of hepatitis C virus (HCV) polyproteins essential for viral replication. By inhibiting NS3/4A protease activity with high potency, telaprevir disrupts maturation of viral proteins and suppresses replication of HCV genotype 1. Additionally, telaprevir interacts with organic anion transporters 1B1 and 2B1, which may influence its pharmacokinetic profile. |
|---|---|
| Mechanism of action | Telaprevir is a NS3/4a protease inhibitor used to inhibit viral HCV replication. NS3/4a protease is an integral part of viral replication and mediates the cleavage the virally encoded polyprotein to mature proteins (NS4A, NS4B, NS5A and NS5B). Telaprevir inhibits NS3/4A with an IC50 of 10nM. |
| Pharmacodynamics | Telaprevir is classified as a direct-acting antiviral (DAA) and prevents viral replication in HCV genotype 1. |
Targets
| Target | Organism | Actions |
|---|---|---|
| NS3/4A protein | Hepatitis C Virus | inhibitor |
| Solute carrier organic anion transporter family member 1B1 | Humans | inhibitor |
| Solute carrier organic anion transporter family member 2B1 | Humans | inhibitor |
ADME / PK
| Absorption | Telaprevir reaches peak plasma concentration 4-5hours after administration. Absolute bioavailability has not been determined. When taken with a normal fat meal (21g of fat), exposure increases by 235% compared to fasting conditions. With low (3.6g of fat) and high fat (56g of fat) meals, exposure increased 117% and 330% respectively. |
|---|---|
| Half-life | Telaprevir has a half-life of elimination of 4.0-4.7 hours after a single dose and an effective half life of 9-11 hours at steady state. |
| Protein binding | Telapravir is 59-76% bound to human plasma proteins following a single dose. It binds to both human serum albumin and α1-acid glycoprotein. |
| Metabolism | Telaprevir is extensively metabolized via hydrolysis, oxidation, and reduction. The major metabolites of Telaprevir are pyrazinoic acid, a metabolite that underwent reduction at the α-ketoamide bond, and the R-diastereomer of telaprevir which is 30-fold less active than the parent compound were found to be the predominant metabolites. The primary enzyme involved in the metabolism of Telaprevir is CYP3A4. Some metabolism is performed by aldo-keto reductases and other reductases. |
| Route of elimination | Telaprevir is mainly eliminated in the feces (82%) with a smaller amount eliminated via expiration (9%) and very little in the urine (1%). 31.9% and 18.8% of drug in the feces was present as the parent compound and R-diastereomer of the parent compound respectively. |
| Volume of distribution | The estimated apparent volume of distribution for Telapravir is 252 litres with an inter-individual variability of 72%. |
| Clearance | Telaprevir has an estimated aparent total body clearance of 32.4 liters per hour with an interindividual variability of 27.2%. |
Formulation & handling
- Telaprevir is a small molecule oral formulation with limited water solubility, requiring consideration for dissolution enhancement in tablets.
- Its peptide-like structure indicates potential sensitivity to enzymatic degradation, supporting oral dosing with protective film coatings.
- Avoid concomitant use with St. John's Wort due to significant interaction reducing telaprevir plasma levels.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed in the US, Canada, and EU, with key US patents expiring between 2021 and 2028, indicating a progressing market maturity phase with potential for generic competition. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Telaprevir is marketed under multiple branded names across the US, Canada, and EU, indicating a broad global presence. The originator companies hold several US patents with expiration dates ranging from 2021 to 2028, suggesting that generic competition has already begun or will emerge progressively as patents expire. This phased patent expiry supports a transitioning supply landscape from branded to generic sources. |
|---|
Safety
| Toxicity | Serious skin reactions, including Stevens Johnson Syndrome, Drug Reaction with Eosinophilia and Systemic Symptoms, and Toxic Epidermal Necrolysis, have been reported in patients treated with telaprevir combination treatment. Use of [DB00811], [DB00008], [DB00022] and Telaprevir is associated with a further increase in anemia frequency than in [DB00811], [DB00008], and [DB00022] without telaprevir. |
|---|
- Handling requires appropriate protective measures to prevent skin exposure due to the potential for severe cutaneous adverse reactions
- Combined use with APIs , , and may increase the risk of hematologic toxicity, including anemia
- Use in manufacturing and formulation should consider the heightened toxicity profile when telaprevir is present with related antiviral compounds
Telaprevir is a type of Anti-HCV agents
Anti-HCV agents, belonging to the pharmaceutical API category, are potent medications used in the treatment of Hepatitis C Virus (HCV) infection. Hepatitis C is a viral disease that affects the liver and can lead to severe health complications if left untreated. Anti-HCV agents work by targeting specific mechanisms involved in the replication and spread of the HCV virus within the body.
These pharmaceutical APIs are designed to inhibit various steps of the viral lifecycle, including viral entry into liver cells, viral RNA replication, and assembly of new viral particles. By disrupting these critical processes, anti-HCV agents effectively reduce the viral load in the body, slow down disease progression, and ultimately improve patient outcomes.
The development of anti-HCV agents has revolutionized the management of HCV infection, offering new hope for patients. These APIs are often used in combination with other antiviral drugs to form highly effective treatment regimens known as direct-acting antiviral (DAA) therapies. DAAs have significantly higher cure rates compared to older treatment options, such as interferon-based therapies, and are associated with fewer side effects.
The pharmaceutical industry has made significant advancements in the development of anti-HCV agents, resulting in a diverse range of APIs with varying mechanisms of action. This diversity allows healthcare professionals to tailor treatment plans based on the specific characteristics of each patient's HCV infection, maximizing the chances of successful viral eradication.
In summary, anti-HCV agents are a crucial category of pharmaceutical APIs used in the treatment of Hepatitis C. Their targeted action against the HCV virus has revolutionized the management of this chronic infection, providing more effective and better-tolerated treatment options for patients.
Telaprevir API manufacturers & distributors
Compare qualified Telaprevir API suppliers worldwide. We currently have 1 companies offering Telaprevir 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 |
|---|---|---|---|---|---|
| Shanghai Acebright | Producer | China | China | CoA | 23 products |
When sending a request, specify which Telaprevir 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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