GEM-231

Identification

Generic Name
GEM-231
DrugBank Accession Number
DB05798
Background

GEM231 is a second-generation antisense oligonucleotide targeting the mRNA of the R1alpha regulatory subunit of cAMP dependent protein kinase. A monoclonal antibody combined with a toxic substance that is used treat certain types of acute myeloid leukemia in older patients and is being studied in the treatment of other types of cancer. Monoclonal antibodies are made in the laboratory and can locate and bind to cancer cells.

Type
Biotech
Groups
Investigational
Biologic Classification
Gene Therapies
Antisense oligonucleotides
Synonyms
Not Available
External IDs
  • GEM 231
  • GEM-231
  • GEM231
  • HYBO165

Pharmacology

Indication

Investigated for use/treatment in solid tumors.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Pharmacodynamics

Not Available

Mechanism of action

GEM-231 has also demonstrated potentiation of the effects of certain conventional cytotoxic chemotherapy drugs. Hybridon is conducting studies of the DNA methyltransferase gene and has identified specific sequences on mRNA as targets for chemically-modified antisense oligonucleotides.

TargetActionsOrganism
UcAMP-dependent protein kinase type II-alpha regulatory subunitNot AvailableHumans
UcAMP-dependent protein kinase type I-alpha regulatory subunitNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

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
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
255810-66-3

References

General References
  1. Goel S, Desai K, Macapinlac M, Wadler S, Goldberg G, Fields A, Einstein M, Volterra F, Wong B, Martin R, Mani S: A phase I safety and dose escalation trial of docetaxel combined with GEM231, a second generation antisense oligonucleotide targeting protein kinase A R1alpha in patients with advanced solid cancers. Invest New Drugs. 2006 Mar;24(2):125-34. [Article]
  2. Blay J: GEM-231 (Hybridon). IDrugs. 2000 Sep;3(9):1075-80. [Article]
PubChem Substance
347910237

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Regulatory subunit of the cAMP-dependent protein kinases involved in cAMP signaling in cells. Type II regulatory chains mediate membrane association by binding to anchoring proteins, including the ...
Gene Name
PRKAR2A
Uniprot ID
P13861
Uniprot Name
cAMP-dependent protein kinase type II-alpha regulatory subunit
Molecular Weight
45518.015 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Regulatory subunit of the cAMP-dependent protein kinases involved in cAMP signaling in cells.
Gene Name
PRKAR1A
Uniprot ID
P10644
Uniprot Name
cAMP-dependent protein kinase type I-alpha regulatory subunit
Molecular Weight
42981.28 Da

Drug created on November 18, 2007 18:27 / Updated on June 12, 2020 16:52