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MedKoo product information:
LE-DT
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MedKoo Code#: 205512
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Name: LE-DT
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CAS#: 114977-28-5
Synonym: LE-DT
(Liposome Encapsulated Docetaxel); docetaxel
liposome; liposomal-encapsulated docetaxel; liposome
entrapped docetaxel; Abbreviation: LE-DT.
IUPAC/Chemical name:
(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b-diyl
diacetate.
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Chemical structure: |
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Docetaxel
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Theoretical analysis: |
Chemical Formula: C45H55NO15
Exact Mass: 849.35717
Molecular Weight: 849.91590
Elemental Analysis: C, 63.59; H, 6.52; N, 1.65; O, 28.24
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Availability and price:
This agent
is not in stock, which may be available through custom synthesis.
To inquire quotation and lead time or to ask questions, please send email to
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Information about this agent
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liposomal docetaxel (LE-DT)
is a formulation of the poorly soluble, semi-synthetic,
second-generation taxane docetaxel encapsulated within liposomes, with
antineoplastic activity. Upon intravenous administration, docetaxel
binds to and stabilizes tubulin, thereby inhibiting microtubule
disassembly which results in cell-cycle arrest at the G2/M phase and
cell death. This liposomal formulation solubilizes docetaxel without the
use of toxic solvents such as Tween 80, permitting the administration of
larger doses of docetaxel while avoiding solvent-associated toxicity,
including hypersensitivity reactions. In addition, liposomal delivery of
docetaxel improves drug penetration into tumors and decreases drug
clearance, thereby increasing the duration of therapeutic drug effects
while lowering the toxicity profile. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer:
NeoPharm, Inc.
1: Pohlen U, Buhr HJ, Berger G. Improvement of
biodistribution with PEGylated liposomes containing docetaxel with
degradable starch microspheres for hepatic arterial infusion in the
treatment of liver metastases: a study in CC-531 liver tumor-bearing WAG
RIJ rats. Anticancer Res. 2011 Jan;31(1):153-9. PubMed PMID: 21273593.
2: Nagykálnai T. [Non-pegylated doxorubicin (Myocet®) as the less
cardiotoxic alternative of free doxorubicin]. Magy Onkol. 2010
Dec;54(4):359-67. Review. Hungarian. PubMed PMID: 21163767.
3: Zhai G, Wu J, Yu B, Guo C, Yang X, Lee RJ. A transferrin
receptor-targeted liposomal formulation for docetaxel. J Nanosci
Nanotechnol. 2010 Aug;10(8):5129-36. PubMed PMID: 21125861.
4: Antón A, Ruiz A, Plazaola A, Calvo L, Seguí MA, Santaballa A, Muñoz
M, Sánchez P, Miguel A, Carrasco E, Lao J, Camps J, Alfaro J, Antolín S,
Cámara MC. Phase II clinical trial of liposomal-encapsulated doxorubicin
citrate and docetaxel, associated with trastuzumab, as neoadjuvant
treatment in stages II and IIIA HER2-overexpressing breast cancer
patients. GEICAM 2003-03 study. Ann Oncol. 2011 Jan;22(1):74-9. Epub
2010 Jul 5. PubMed PMID: 20603435.
5: Zhai G, Wu J, Xiang G, Mao W, Yu B, Li H, Piao L, Lee LJ, Lee RJ.
Preparation, characterization and pharmacokinetics of folate
receptor-targeted liposomes for docetaxel delivery. J Nanosci
Nanotechnol. 2009 Mar;9(3):2155-61. PubMed PMID: 19435095.
6: Huynh NT, Passirani C, Saulnier P, Benoit JP. Lipid nanocapsules: a
new platform for nanomedicine. Int J Pharm. 2009 Sep 11;379(2):201-9.
Epub 2009 May 4. Review. PubMed PMID: 19409468.
7: Antón A, Ruiz A, Seguí MA, Calvo L, Muñoz M, Lao J, Sancho F,
Fernández L. Phase I clinical trial of liposomal-encapsulated
doxorubicin citrate and docetaxel, associated with trastuzumab, as
neo-adjuvant treatment in stages II and IIIA, HER2-overexpressing breast
cancer patients. GEICAM 2003-03 study. Ann Oncol. 2009 Mar;20(3):454-9.
Epub 2008 Dec 11. PubMed PMID: 19074216.
8: Yuan WM, Song QG, Zhang ZR, Fu Y, Liu J, He Q. LHRHa aided liposomes
targeting to human ovarian tumor cells: preparation and cellular uptake.
Pharmazie. 2008 Jun;63(6):434-8. PubMed PMID: 18604986.
9: Hwang SH, Rait A, Pirollo KF, Zhou Q, Yenugonda VM, Chinigo GM, Brown
ML, Chang EH. Tumor-targeting nanodelivery enhances the anticancer
activity of a novel quinazolinone analogue. Mol Cancer Ther. 2008
Mar;7(3):559-68. PubMed PMID: 18347143.
10: Merritt WM, Lin YG, Spannuth WA, Fletcher MS, Kamat AA, Han LY,
Landen CN, Jennings N, De Geest K, Langley RR, Villares G, Sanguino A,
Lutgendorf SK, Lopez-Berestein G, Bar-Eli MM, Sood AK. Effect of
interleukin-8 gene silencing with liposome-encapsulated small
interfering RNA on ovarian cancer cell growth. J Natl Cancer Inst. 2008
Mar 5;100(5):359-72. Epub 2008 Feb 26. PubMed PMID: 18314475; PubMed
Central PMCID: PMC2770251.
11: Dhanikula AB, Lafleur M, Leroux JC. Characterization and in vitro
evaluation of spherulites as sequestering vesicles with potential
application in drug detoxification. Biochim Biophys Acta. 2006
Nov;1758(11):1787-96. Epub 2006 Aug 17. PubMed PMID: 16999932.
12: Mrózek E, Rhoades CA, Allen J, Hade EM, Shapiro CL. Phase I trial of
liposomal encapsulated doxorubicin (Myocet; D-99) and weekly docetaxel
in advanced breast cancer patients. Ann Oncol. 2005 Jul;16(7):1087-93.
Epub 2005 Apr 22. PubMed PMID: 15849219.
13: Dunton CJ. New options for the treatment of advanced ovarian cancer.
Semin Oncol. 1997 Feb;24(1 Suppl 5):S5-2-S5-11. Review. PubMed PMID:
9122739.
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