Details of the Drug

General Information of Drug (ID: DMNHPOT)

Drug Name
LErafAON
Synonyms
RafAON; Antisense raf oligonucleotide, NeoPharm; LErafAON, Insys; LErafAON-ETU; Liposomal antisense therapy, NeoPharm; Cancer therapeutic (antisense), NeoPharm; Liposome encapsulated c-raf antisense oligodeoxynucleotide, NeoPharm; Antisense oligonucleotides (liposome-encapsulated), NeoPharm
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [1], [2]
Drug Type
Antisense drug
ADMET Property
Half-life
The concentration or amount of drug in body reduced by one-half in 30.36 +/- 23.87 hours [3]
Cross-matching ID
DrugBank ID
DB04973
TTD ID
D0W9QI

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Raf messenger RNA (Raf mRNA) TTAN5W2 RAF1_HUMAN Not Available [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Solid tumour/cancer
ICD Disease Classification 2A00-2F9Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Raf messenger RNA (Raf mRNA) DTT RAF1 2.12E-04 0.49 2.78
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

References

1 ClinicalTrials.gov (NCT00100672) Study to Determine the Maximum Tolerated Dose of LErafAON in Patients With Advanced Cancer. U.S. National Institutes of Health.
2 Delivery of a liposomal c-raf-1 antisense oligonucleotide by weekly bolus dosing in patients with advanced solid tumors: a phase I study. Clin Cancer Res. 2004 Nov 1;10(21):7244-51.
3 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4 Combination with liposome-entrapped, ends-modified raf antisense oligonucleotide (LErafAON) improves the anti-tumor efficacies of cisplatin, epirubicin, mitoxantrone, docetaxel and gemcitabine. Anticancer Drugs. 2004 Mar;15(3):243-53.
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2184).
6 Clinical pipeline report, company report or official report of Roche.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009).
9 Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32.
10 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
11 Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.