Tigapotide
Identification
- Generic Name
- Tigapotide
- DrugBank Accession Number
- DB04985
- Background
Tigapotide is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid.
- Type
- Biotech
- Groups
- Investigational
- Biologic Classification
- Protein Based Therapies
Other protein based therapies - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>PCK3145 (PSP-94 [31-45]) Sequence PGDSTRKCMDLKGNK
Download FASTA Format- Synonyms
- Tigapotide
- External IDs
- PCK-3145
- PCK3145
Pharmacology
- Indication
For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.
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- Pharmacodynamics
PCK3145 is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is down regulated in patients with advanced prostate cancer, and believed to be a survival mechanism for the cancer cells. Results from an earlier trial conducted in the U.K. showed PCK3145 to be safe and well tolerated at all doses tested and further suggest that it also plays a role in preventing the metastatic process as measured by its effect on MMP-9 levels, a Gelatinase B enzyme involved in angiogenesis, tumor invasion and metastasis.
- Mechanism of action
The mechanism of action and receptor for PCK3145 suggests PCK3145 to be a signal transduction inhibitor with multiple ways (apoptosis, anti-angiogenesis and anti-metastasis) to restrict disease development.
Target Actions Organism U40S ribosomal protein SA Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
0.35 hours to 1.45 hours
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Non-clinical toxicology studies in mice and primates indicated that a treatment for 28 consecutive days by intravenous administration of PCK3145 up to 450 mg/kg/day in mice and 25 mg/kg/day in primates resulted in no clear evidence of toxicity.
- 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.Not Available
- Food Interactions
- Not Available
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
- 1WZ6S45S94
- CAS number
- 848084-83-3
References
- General References
- Shukeir N, Arakelian A, Chen G, Garde S, Ruiz M, Panchal C, Rabbani SA: A synthetic 15-mer peptide (PCK3145) derived from prostate secretory protein can reduce tumor growth, experimental skeletal metastases, and malignancy-associated hypercalcemia. Cancer Res. 2004 Aug 1;64(15):5370-7. [Article]
- Annabi B, Bouzeghrane M, Currie JC, Hawkins R, Dulude H, Daigneault L, Ruiz M, Wisniewski J, Garde S, Rabbani SA, Panchal C, Wu JJ, Beliveau R: A PSP94-derived peptide PCK3145 inhibits MMP-9 secretion and triggers CD44 cell surface shedding: implication in tumor metastasis. Clin Exp Metastasis. 2005;22(5):429-39. [Article]
- Hawkins RE, Daigneault L, Cowan R, Griffiths R, Panchal C, Armstrong A, Fenemore J, Irvine A, Sereda K, Dulude H: Safety and tolerability of PCK3145, a synthetic peptide derived from prostate secretory protein 94 (PSP94) in metastatic hormone-refractory prostate cancer. Clin Prostate Cancer. 2005 Sep;4(2):91-9. [Article]
- External Links
- PubChem Substance
- 347909874
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Treatment Prostate Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Virus receptor activity
- Specific Function
- Required for the assembly and/or stability of the 40S ribosomal subunit. Required for the processing of the 20S rRNA-precursor to mature 18S rRNA in a late step of the maturation of 40S ribosomal s...
- Gene Name
- RPSA
- Uniprot ID
- P08865
- Uniprot Name
- 40S ribosomal protein SA
- Molecular Weight
- 32853.79 Da
References
- Annabi B, Currie JC, Bouzeghrane M, Dulude H, Daigneault L, Garde S, Rabbani SA, Panchal C, Wu JJ, Beliveau R: Contribution of the 37-kDa laminin receptor precursor in the anti-metastatic PSP94-derived peptide PCK3145 cell surface binding. Biochem Biophys Res Commun. 2006 Jul 21;346(1):358-66. Epub 2006 Jun 2. [Article]
Drug created at October 21, 2007 22:23 / Updated at February 21, 2021 18:51