Stereochemistry | ACHIRAL |
Molecular Formula | C31H28N4O4 |
Molecular Weight | 520.5784 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C1N(CCNCCCNCCN2C(=O)C3=CC=CC4=CC=CC(C2=O)=C34)C(=O)C5=C6C(C=CC=C16)=CC=C5
InChI
InChIKey=QUNOQBDEVTWCTA-UHFFFAOYSA-N
InChI=1S/C31H28N4O4/c36-28-22-10-1-6-20-7-2-11-23(26(20)22)29(37)34(28)18-16-32-14-5-15-33-17-19-35-30(38)24-12-3-8-21-9-4-13-25(27(21)24)31(35)39/h1-4,6-13,32-33H,5,14-19H2
Elinafide (LU 79553) is a bisintercalating naphthalamide and a topoisomerase II inhibitor has demonstrated a higher binding affinity for DNA and significant antitumour efficacy against a panel of established tumour cell lines, including several multidrug resistant-positive sublines. Elinafide had been in phase II clinical trial for the treatment of ovarian cancer and phase I trials for the treatment of various solid tumours. The major haematological toxicities observed were anaemia and neutropenia. The major non-haematological toxicities observed in the 3-weekly schedule were neuro-muscular presenting clinically as a mixed syndrome of severe weakness (sometimes with pain in both legs), myalgia and arthralgia, asthenia/fatigue/malaise. One fatality was considered related to LU 79553, as the patient had fever and neutropenia. Clinical study of this drug candidate was discontinued due to its neuromuscular dose-limiting toxicity.
Originator
Approval Year
Cmax
AUC
T1/2
Doses
AEs
Sourcing
PubMed
Sample Use Guides
100 mg/m(2)/course (60 min infusion in 500 ml normal saline) (3-weekly regimen)
Route of Administration:
Intravenous