NAV

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
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Pharmacology

Indication

For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.

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Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
U40S ribosomal protein SANot AvailableHumans
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
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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
  1. 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]
  2. 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]
  3. 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]
PubChem Substance
347909874

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentProstate Cancer1

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

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Details1. 40S ribosomal protein SA
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
  1. 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