Exatecan mesylate
[CAS# 169869-90-3]

Identification

• Classification: API >> Other chemicals
• Name: Exatecan mesylate
• Synonyms: DX 8951f; (10S,23S)-23-amino-10-ethyl-18-fluoro-10-hydroxy-19-methyl-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaene-5,9-dione;methanesulfonic acid
• Molecular Formula: C₂₄H₂₂FN₃O₄.CH₄O₃S
• Molecular Weight: 531.55
• CAS Registry Number: 169869-90-3
• EC Number: 881-303-2
• SMILES: CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C5[C@H](CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)N)O.CS(=O)(=O)O

Safety Data

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	3	H301

Discovery and Applications

Exatecan mesylate, a semi-synthetic derivative of the natural product camptothecin, was developed as part of a research program focused on identifying novel anticancer agents. It was synthesized in the late 20th century by scientists at Pfizer, building upon the structure of camptothecin to improve its pharmacokinetic and therapeutic properties.

Exatecan mesylate, a semi-synthetic derivative of camptothecin, exhibits potent antitumor activity against a variety of solid tumors, including ovarian, lung, and colorectal cancers. As a topoisomerase I inhibitor, exatecan mesylate interferes with DNA replication and repair, leading to DNA damage and apoptosis in cancer cells. Clinical studies have demonstrated the efficacy of exatecan mesylate as a single agent or in combination with other chemotherapy drugs in the treatment of advanced or metastatic cancers that have failed conventional therapies. Exatecan mesylate has shown promising results in terms of tumor response rates, progression-free survival, and overall survival, particularly in patients with platinum-resistant ovarian cancer or relapsed/refractory small cell lung cancer. Additionally, exatecan mesylate has been investigated in preclinical models and early-phase clinical trials for its potential in overcoming multidrug resistance and enhancing the efficacy of other anticancer agents.

References

1995. A New Water-soluble Camptothecin Derivative, DX-8951f, Exhibits Potent Antitumor Activity against Human Tumors in vitro and in vivo. Japanese journal of cancer research : Gann, 86(8).
DOI: 10.1111/j.1349-7006.1995.tb02468.x

2008. Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma. Expert Review of Anticancer Therapy, 8(5).
DOI: 10.1586/14737140.8.5.819

2016. Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads. Bioorganic & Medicinal Chemistry Letters, 26(6).
DOI: 10.1016/j.bmcl.2016.02.020