Identification

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Name
GEM-231
Accession Number
DB05798
Type
Biotech
Groups
Investigational
Biologic Classification
Gene Therapies
Antisense oligonucleotides
Description

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.

Synonyms
Not Available
External IDs
GEM 231 / GEM-231 / GEM231 / HYBO165
Categories
UNII
Not Available
CAS number
255810-66-3

Pharmacology

Indication

Investigated for use/treatment in solid tumors.

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
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

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. [PubMed:16683205]
  2. Blay J: GEM-231 (Hybridon). IDrugs. 2000 Sep;3(9):1075-80. [PubMed:16049867]
External Links
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

Taxonomy

Classification
Not classified

Targets

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 11:27 / Updated on June 04, 2019 06:19