MedKoo's Product: Heptaplatin

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MedKoo product information:

Heptaplatin

MedKoo Code#: 100422

Name: Heptaplatin

CAS#: 146665-77-2

Synonym: Eptaplatin, Heptaplatin, Sunpla; NSC-644591, NSC-D-644591, SKI-2053R. Chemical name: **cis-[(4R,5R)-2-Isopropyl-1,3-dioxolane-4,5-bis(methylamine)-N,N'][malonato(2-)-O,O']platinum; **(SP-4-2)-[(4R,5R)-2-Isopropyl-1,3-dioxolane-4,5-bis(methanamine)-N,N'][propanedioato(2-)-O,O']platinum

IUPAC/Chemical name:

[SP-4-2-[4R-(2a,4a,5b)]]-[2-(1-Methylethyl)-1,3-dioxolane-4,5-dimethanamine-N,N'][propanedioato(2-)-O,O']-platinum

Chemical structure:

Theoretical analysis :

Chemical Formula: C11H20N2O6Pt

Exact Mass: 471.09691

Molecular Weight: 471.37

m/z: 471.09691 (100.0%), 470.09480 (97.4%), 472.09707 (74.6%), 474.10001 (21.2%), 472.10027 (11.9%), 471.09816 (11.6%), 473.10043 (8.9%), 475.10337 (2.5%), 468.09317 (2.3%), 473.10116 (1.2%), 472.09905 (1.2%)

Elemental Analysis: C, 28.03; H, 4.28; N, 5.94; O, 20.37; Pt, 41.39

Availability and price:

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Quality control data:

Product will be shipped with supporting analytical data.

Information about this agent

Heptaplatin (HTP), a newly developed platinum analog, has been approved for the treatment of gastric cancers in South Korea. The anti-proliferative activity of HTP was evaluated in FaDu, a human HNSCC cell line. Combinations of HTP with 5-fluorouracil (5-FU) or paclitaxel (PTX) were determined using combination indexes, and were compared with combinations of cisplatin and 5-FU or PTX. In order to evaluate the transport of HTP into tumor tissue, its penetration through multicell layers (MCLs) of cancer cells was measured. Cisplatin+5-FU and HTP+5-FU showed additive to antagonistic interactions. In terms of the HTP+paclitaxel combination, HTP showed antagonism and additivity at the 50 and 80% growth inhibition levels, respectively. An additive interaction was obtained and apoptosis was increased by 2-fold at both inhibition levels when the combinatorial PTX dose was reduced to 1/10. HTP, but not cisplatin or oxaliplatin (L-OHP), maintained its anti-proliferative activity after MCL penetration at clinically relevant concentrations, which can be attributed to lower protein binding of HTP. The results suggest that low-dose PTX may sensitize tumor cells to HTP. HTP also showed greater penetration through multilayers of tumor cells compared to cisplatin and L-OHP, which may be an important characteristic for solid tumor treatment. Overall, the research results support the clinical development of HTP in combination with low-dose PTX against HNSCC. see Anticancer Drugs. 2006 Apr;17(4):377-84.

References

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20: Cho YB, Kim DK, Kim KH, Miyamoto G. Pharmacokinetics of cis-malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane]platinum(II) in rats. Arzneimittelforschung. 1996 Jun;46(6):629-34. PubMed PMID: 8767356.

21: Cho YB, Kim KH, Kim DK. Pharmacokinetics, tissue distribution, and excretion of cis-malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3- dioxolane]platinum(II) in dogs. Drug Metab Dispos. 1995 Nov;23(11):1280-5. PubMed PMID: 8591731.

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24: Kim DK, Kim HT, Tai JH, Cho YB, Kim TS, Kim KH, Park JG, Hong WS. Pharmacokinetics and antitumor activity of a new platinum compound, cis-malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1, 3- dioxolane]platinum(II), as determined by ex vivo pharmacodynamics. Cancer Chemother Pharmacol. 1995;37(1-2):1-6. PubMed PMID: 7497577.

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