DRF-1042

• CAT Number: I006542
• CAS Number: 200619-13-2
• PubChem Substance ID: 23631031
• Molecular Formula: C22H20N2O6
• Molecular Weight: 408.41
• Purity: 98%
• Target: topoisomerase I inhibitor
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term or -20 °C for long term
• IUPAC Name: (19S)-19-ethyl-19-hydroxy-12-(2-hydroxyethoxy)-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
• InChI: InChI=1S/C22H20N2O6/c1-2-22(28)15-10-17-18-13(9-12-5-3-4-6-16(12)23-18)20(29-8-7-25)24(17)19(26)14(15)11-30-21(22)27/h3-6,9-10,20,25,28H,2,7-8,11H2,1H3/t20?,22-/m0/s1
• InChIKey: XAKLYHGHEFMDAP-IAXKEJLGSA-N
• SMILES: CCC1(C2=C(COC1=O)C(=O)N3C(C4=CC5=CC=CC=C5N=C4C3=C2)OCCO)O

DRF-1042(CAT: I006542)is a DNA topoisomerase I inhibitor. It is being investigated as a potential treatment for solid tumors. DNA topoisomerase I is an enzyme involved in DNA replication and transcription by relieving torsional strain in DNA. Inhibition of this enzyme can disrupt DNA processes and lead to cell death, making it an attractive target for cancer therapy. DRF-1042 shows promise in preclinical studies and may have potential as a therapeutic agent for the treatment of solid tumors. Further research is ongoing to evaluate its efficacy and safety profile.

Overview of Clinical Research

OriginatorDr: Reddys Laboratories
Class:Antineoplastics; Camptothecins; Small molecules
Mechanism of Action: DNA topoisomerase I inhibitors
Orphan Drug Status:No

Reference

1:Safety, tolerability, and pharmacokinetics of a capsule formulation of DRF-1042, a novel camptothecin analog, in refractory cancer patients in a bridging phase I study. Chatterjee A, Digumarti R, Katneni K, Upreti VV, Mamidi RN, Mullangi R, Surath A, Srinivas ML, Uppalapati S, Jiwatani S, Srinivas NR.J Clin Pharmacol. 2005 Apr;45(4):453-60. PMID: 15778426
2:Safety, tolerability, pharmacokinetics, and pharmacodynamics of an orally active novel camptothecin analog, DRF-1042, in refractory cancer patients in a phase I dose escalation study. Chatterjee A, Digumarti R, Mamidi RN, Katneni K, Upreti VV, Surath A, Srinivas ML, Uppalapati S, Jiwatani S, Subramaniam S, Srinivas NR.J Clin Pharmacol. 2004 Jul;44(7):723-36. PMID: 15199077
3:Quantitative determination of DRF-1042 in human plasma by HPLC: validation and application in clinical pharmacokinetics. Upreti VV, Mamidi RN, Katneni K, Srinivas NR.Biomed Chromatogr. 2003 Sep;17(6):385-90. PMID: 13680849