Raltitrexed

Bezeichnung:Raltitrexed

CAS-Nr112887-68-0

Englisch Name:Raltitrexed

CBNumberCB1222070

SummenformelC21H22N4O6S

Molgewicht458.49

MOL-Datei112887-68-0.mol

Raltitrexed physikalisch-chemischer Eigenschaften

Schmelzpunkt	176-1800C
Dichte	1.49±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	H2O: ≥10mg/mL
Aggregatzustand	solid
pka	3.50±0.10(Predicted)
Farbe	off-white to light yellow
InChIKey	IVTVGDXNLFLDRM-HNNXBMFYSA-N
CAS Datenbank	112887-68-0(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi,T
R-Sätze:	36/38-25-61
S-Sätze:	26-37/39-45-53
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	2
HS Code	2934.99.4700

Gefahreninformationscode (GHS)

Raltitrexed Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/38:Reizt die Augen und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Beschreibung
Tomudex was launched in Ireland, France, Luxembourg and the UK for advanced colorectal cancer and it was prepared in a convergent manner (6 steps) from diethyl L-glutamate and 6-bromomethyi-2-methyl-quinazolin4(3H)-one. Tomudex is a highly selective inhibitor of thymidylate synthase (TS), the key enzyme in the biochemical conversion of dUMP to dTMP. It enters the cell via the reduced folatefmethotrexate cell membrane carrier and is converted to the polyglutamate species by folylpolyglutamate synthase within 4h where it then binds to the folate substrate site of TS. Clinically, it had a 29% response rate in patients with advanced colorectal cancer. It is water soluble, can be administered as a single dose every three weeks and had no hepto- or nephrotoxicity.
Chemische Eigenschaften
Yellow Crystalline Powder
Originator
Zeneca (UK)
Verwenden
Folate-based inhibitor of thymidylate synthase; rapidly and extensively metabolized to its more potent polyglutamate derivatives. Antineoplastic
Definition
ChEBI: ICI D1694 is a N-acyl-amino acid.
Trademarks
Tomudex (Zeneca).
Biochem/physiol Actions
Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
Clinical Use
Treatment of colorectal cancer when fluorouracil and folinic acid cannot be used
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine, increased risk of agranulocytosis.
Folic and folinic acid: impairs cytotoxic action - avoid.
Stoffwechsel
Raltitrexed is actively transported into cells and metabolised to active polyglutamate forms.
The remainder of a dose is not metabolised and is excreted unchanged, about 50% of a dose appearing in the urine, and about 15% in the faeces.

Raltitrexed Upstream-Materialien And Downstream Produkte

Raltitrexed Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

112887-68-0, Raltitrexed Verwandte Suche:

Send Inquriy