Satraplatin Struktur

Satraplatin

Bezeichnung:Satraplatin

CAS-Nr129580-63-8

Englisch Name:Satraplatin

CBNumberCB2675796

SummenformelC10H20Cl2N2O4Pt

Molgewicht498.26

MOL-Datei129580-63-8.mol

Satraplatin physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	DMF: 0.16 mg/mL; DMSO: 0.5 mg/mL
Aggregatzustand	Powder
Farbe	Off-white to yellow

Sicherheit

Toxizität

LD50 in mice (mg/kg): 30 i.p.; 330 orally (Kelland)

Gefahreninformationscode (GHS)

Satraplatin Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Antineoplastic.
Definition
ChEBI: A platinum coordination entity that consists of a central platunum atom bound to chloro (x2), acetate (x2), amino, and cyclohexylamino groups. Used for treatment of advanced prostate cancer.
Pharmazeutische Anwendungen
Satraplatin (JM216, cis,trans,cis-[PtCl2(OAc)2(NH3)(C6H5NH2)]) is a Pt(IV) or Pt4+ complex, which is active by oral administration, as it is more hydrophobic than cisplatin. This form of administration is very attractive because of the convenience and freedom it provides to the patient. Satraplatin also has a milder toxicity profile and is shows no cross-resistance with cisplatin. Satraplatin in combination with prednisone has completed phase III clinical trials against hormone-refractory prostate cancer. The results were very encouraging, but the overall survival rate did not improve significantly enough. As a result, the fast-track approval of the FDA was not granted.
Structurally, satraplatin consists of a Pt(IV) centre, which is coordinated by six ligands forming a close to octahedral geometry. In general, octahedral Pt(IV) complexes (low-spin d6) are much more kinetically inert than square planar Pt(II) complexes.
Clinical Use
This newest organometallic agent currently is in clinical trials as a second-line agent for the treatment of hormone-refractory prostate cancer . There is hope that it also will find value in ovarian cancer and small cell lung cancer.
Nebenwirkungen
As with other organoplatinum complexes, the diaquo form is active. At this early stage, the toxicity profile appears to be mild, with dose-related myelosuppression, particularly neutropenia and thrombocytopenia, being the major use-limiting side effect.
Stoffwechsel
Unlike the square-planar Pt(II) complexes currently on the market, it is active by the oral route. It is metabolized quickly in whole blood, producing up to six metabolites. The major metabolite is the desacetoxy analogue.

Satraplatin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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