AVN-944

Identification

Generic Name
AVN-944
DrugBank Accession Number
DB05500
Background

AVN944 is a biotech drug that demonstrated a statistically meaningful impact on IMPDH and other proteins that are critical to activities in cancer cells, including nucleotide biosynthesis, energy and metabolism, DNA replication, apoptosis and cell cycle control. AVN944 has been associated with cancer cell death in clinical trials. It is being investigated for the treatment of patients with advanced hematologic malignancies.

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
>>uniprot|Q9RHG1|Q9RHG1_BACCE IMPDH.
MWESKFVKEGLTFDDVLLVPAKSDVLPREVSVKTVLSESLQLNIPLISAGMDTVTEADMA
IAMARQGGLGIIHKNMSIEQQAEQVDKVKRSESGVISDPFFLTPEHQVYDAEHLMGKYRI
SGVPVVNNLDERKLVGIITNRDMRFIQDYSIKISDVMTKEQLITAPVGTTLDEAEKILQK
YKIEKLPLVDNNGVLQGLITIKDIEKVIEFPNSAKDKQGRLLVGAAVGVTADAMTRIDAL
VKASVDAIVLDTAHGHSQGVIDKVKEVRAKYPSLNIIAGNVATAEATGALIEAGANVVKV
GIGPGSICTTRVVAGVGVPQLTAVYDCATEARKHGIPVIADGGIKYSGDMVKALAAGAHV
VMLGSMFAGVAESPGETEIYQGRQFKVYRGMGSVGAMEKGSKDRYFQEGNKKLVPEGIEG
RVPYKGPLADTVHQLVGGLRAGMGYCGAQDLEFLRENAQFVRMSGAGLLESHPHHVQITK
EAPTTHYNVLYINRRRFYISVYFFLIMLE
Download FASTA Format
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in cancer/tumors (unspecified), leukemia (unspecified), lymphoma (unspecified), multiple myeloma, and pancreatic cancer.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

IMPDH is highly upregulated in most hematological cancers and in many solid tumors. AVN944 is a biotech drug that demonstrated a statistically meaningful impact in inhibiting IMPDH and other proteins that are critical to activities in cancer cells, including nucleotide biosynthesis, energy and metabolism, DNA replication, apoptosis and cell cycle control. AVN944 has been associated with cancer cell death in clinical trials. It is being investigated for the treatment of patients with advanced hematologic malignancies.

Mechanism of action

AVN944 inhibits IMPDH and appears to induce apoptosis. Specifically, it was found that the gene HspA1A, a marker of stress response found to correlate with depleted GTP pools in cancer cell lines, is induced within hours upon the first treatment of the drug in patients, even at the trial's lowest doses. Following continued dosing of AVN944, this marker of disease cell stress was elevated even in the absence of circulating levels of the drug between doses.

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
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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
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
Not Available

Chemical Identifiers

UNII
I3NPL1V48Q
CAS number
Not Available

References

General References
  1. Chen L, Pankiewicz KW: Recent development of IMP dehydrogenase inhibitors for the treatment of cancer. Curr Opin Drug Discov Devel. 2007 Jul;10(4):403-12. [Article]
  2. Huang M, Ji Y, Itahana K, Zhang Y, Mitchell B: Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41. Epub 2007 Apr 25. [Article]
PubChem Substance
347910175

Clinical Trials

Clinical Trials

Pharmacoeconomics

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

Properties

State
Solid
Experimental Properties
Not Available

Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52