DTS-201 sodium
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer.
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- CAS No.: 372491-73-1
- Formule: C49H64N5NaO18
- Masse moléculaire:1034.04
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Description
In Vivo
DTS-201 (i.v., 15 min, on day 1 and 22) sodium is well tolerated in mice (50 mg/kg, MTD) and rats (40 mg/kg, MTD)[1].
DTS-201 (3.2, 12.8 and 25.6 mg/kg, i.v., once weekly for 7 weeks) sodium shows less cardiotoxicity than Doxorubicin[1].
DTS-201 (40-80 mg/kg, i.v.) sodium has a better therapeutic index than free Doxorubicin in NCI-H1299, PC-3, and MDA-MB-231 xenograft mice[1].
Toxicokinetic variables of DTS-201 sodium in Beagle dogs after a 15-min intravenous infusion of DTS-201 at increasing dose levels
| hERG IC50Dose (mg/kg) | Dose (μmol/kg) | Cmax (μM) | Tmax (min) | AUC(0-t) (h ×μM) |
| 4 | 3.9 | 14.4 | 15 | 5.1 |
| 8 | 7.8 | 42.6 | 15 | 15.7 |
| 16 | 15.5 | 83.6 | 15 | 38.2 |
| 32 | 31.0 | 209 | 15 | 127 |
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