Identification
- Generic Name
- Thymalfasin
- DrugBank Accession Number
- DB04900
- Background
Thymalfasin is a chemically synthesized version of thymosin alpha 1 that is identical to human thymosin alpha 1. Thymosin alpha 1 is an acetylated polypeptide. Thymosin alpha 1 is now approved in 35 developing countries for the treatment of Hepatitis B and C. It is also used to boost the immune response in the treatment of other diseases.
- Type
- Biotech
- Groups
- Investigational
- Biologic Classification
- Protein Based Therapies
Interleukin-based products - Protein Structure
- Protein Chemical Formula
- C129H215N33O55
- Protein Average Weight
- 3108.2755 Da
- Sequences
>Thymalfasin SDAAVDTSSEITTKDLKEKKEVVEEAEN
Download FASTA Format- Synonyms
- Thymalfasin
- Thymosin alpha1 (human)
Pharmacology
- Indication
Indicated as an adjuvant for influenza vaccine in elderly patients and as an adjuvant for both influenza and hepatitis B vaccines in chronic hemodialysis patients who failed to achieve adequate antibody titers from previous immunization.
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- Associated Therapies
- Contraindications & Blackbox Warnings
- Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.
- Pharmacodynamics
Thymalfasin is a 28-amino acid polypeptide produced synthetically but originally isolated from thymosin fraction 5, a bovine thymus extract containing a number of immunologically active peptides. In vitro studies have shown that Thymalfasin can influence T-cell production and maturation, stimulate production of Th1 cytokines such as interferon-gamma and interleukin-2, and activate natural killer cell-mediated cytotoxicity.
- Mechanism of action
The mechanism of action of thymalfasin is not completely understood but is thought to be related to its immunomodulating activities, centered primarily around augmentation of T-cell function. In various in vitro assays, thymosin alpha 1 has been shown to promote T-cell differentiation and maturation; for example, CD4+, CD8+, and CD3+ cells have all been shown to be increased. Thymosin alpha 1 has also been shown to increase production of IFN-g, IL-2, IL-3, and expression of IL-2 receptor following activation by mitogens or antigens, increase NK cell activity, increase production of migratory inhibitory factor (MIF), and increase antibody response to T-cell dependent antigens. Thymosin alpha 1 has also been shown to antagonize dexamethasone-induced apoptosis of thymocytes in vitro. In vivo administration of thymosin alpha 1 to animals immunosuppressed by chemotherapy, tumor burden, or irradiation showed that thymosin alpha 1 protects against cytotoxic damage to bone marrow, tumor progression and opportunistic infections, thereby increasing survival time and number of survivors. Many of the in vitro and in vivo effects of thymosin alpha 1 have been interpreted as influences on either differentiation of pluripotent stem cells to thymocytes or activation of thymocytes into activated T-cells. Thymalfasin also has been shown in vitro to upregulate expression of toll like receptors (TLR) including TLR2 and TLR9 in mouse and human dendritic cells, as well as activate NF-kB and JNK/P38/AP1 pathways. Thymalfasin's activation of dendritic cells provides another possible pathway explaining thymalfasin's immunomodulatory and antiviral effects.
- Absorption
Rapidly absorbed with peak serum levels achieved at approximately 2 hours.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Approximately 2 hours. There is no evidence of accumulation following multiple subcutaneous doses.
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There are no reported instances of deliberate or accidental overdosage in humans. Animal toxicology studies have shown no adverse reactions in single doses up to 20 mg/kg and in repeated doses up to 6 mg/kg/day for 13 weeks, which were the highest doses studied. The highest single dose tested in animals represents 800-times the clinical dose.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareArticaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Benzyl alcohol. Bupivacaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Bupivacaine. Butacaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Butacaine. Butamben The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Butamben. Capsaicin The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Capsaicin. Chloroprocaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Chloroprocaine. Cinchocaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Cinchocaine. Cocaine The risk or severity of methemoglobinemia can be increased when Thymalfasin is combined with Cocaine. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Zadaxin
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- W0B22ISQ1C
- CAS number
- 62304-98-7
References
- Synthesis Reference
Christian Birr, Ulrich Stollenwerk, "Method of preparing thymosin alpha 1 and derivatives thereof." U.S. Patent US4466918, issued April, 1979.
US4466918- General References
- Chien RN, Liaw YF: Thymalfasin for the treatment of chronic hepatitis B. Expert Rev Anti Infect Ther. 2004 Feb;2(1):9-16. [Article]
- Sjogren MH: Thymalfasin: an immune system enhancer for the treatment of liver disease. J Gastroenterol Hepatol. 2004 Dec;19 Suppl 6:S69-72. [Article]
- Liaw YF: Thymalfasin (thymosin-alpha 1) therapy in patients with chronic hepatitis B. J Gastroenterol Hepatol. 2004 Dec;19 Suppl 6:S73-5. [Article]
- Sjogren MH: Thymalfasin: an immune system enhancer for the treatment of liver disease. J Gastroenterol Hepatol. 2004 Dec;19(12):S69-72. [Article]
- Liaw YF: Thymalfasin (thymosin-alpha 1) therapy in patients with chronic hepatitis B. J Gastroenterol Hepatol. 2004 Dec;19(12):S73-5. [Article]
- Vemuri S: Comparison of assays for determination of peptide content for lyophilized thymalfasin. J Pept Res. 2005 Apr;65(4):433-9. [Article]
- Rustgi VK: Thymalfasin for the treatment of chronic hepatitis C infection. Expert Rev Anti Infect Ther. 2005 Dec;3(6):885-92. [Article]
- Rustgi VK: Thymalfasin for the treatment of chronic hepatitis C infection. Ann N Y Acad Sci. 2007 Sep;1112:357-67. Epub 2007 Jun 28. [Article]
- Gramenzi A, Cursaro C, Andreone P, Bernardi M: Thymalfasin: clinical pharmacology and antiviral applications. BioDrugs. 1998 Jun;9(6):477-86. [Article]
- Pierluigi B, D'Angelo C, Fallarino F, Moretti S, Zelante T, Bozza S, De Luca A, Bistoni F, Garaci E, Romani L: Thymosin alpha1: the regulator of regulators? Ann N Y Acad Sci. 2010 Apr;1194:1-5. doi: 10.1111/j.1749-6632.2010.05465.x. [Article]
- External Links
- PubChem Substance
- 46504578
- 38221
- ChEMBL
- CHEMBL2103979
- PharmGKB
- PA164748387
- RxList
- RxList Drug Page
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Cirrhosis of the Liver 2 4 Completed Treatment Sepsis 1 4 Unknown Status Treatment Curable Hepatitis B Virus-Related Hepatocellular Carcinoma 1 3 Completed Treatment Chronic Hepatitis C Virus (HCV) Infection 1 3 Completed Treatment Chronic Hepatitis C Virus (HCV) Infection / Hepatitis C Virus (HCV) Infection 2 3 Completed Treatment Sepsis 1 3 Recruiting Treatment Stage II Colorectal Cancer / Stage III Colorectal Cancer 1 3 Unknown Status Prevention 2019 Novel Coronavirus Infection / Coronavirus Disease 2019 (COVID‑19) 1 2 Active Not Recruiting Prevention Coronavirus Disease 2019 (COVID‑19) 1 2 Completed Supportive Care End Stage Renal Disease (ESRD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous Injection Subcutaneous 1.6 mg/vial Powder 1.6 mg/1ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Drug created at October 21, 2007 22:23 / Updated at January 14, 2023 19:02