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| Home > R&D > Genexol-PM |
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Paclitaxel (TaxolTM, Bristol-Myers Squibb) has demonstrated significant activity in clinical trials against a
variety of human tumors, including ovarian cancer, breast and esophageal cancer, non-small cell lung
cancer, melanoma and leukemias. However, the clinical use of this promising anticancer agent is associated
with several toxic side effects. Because of paclitaxel's poor water solubility, systemic administration of this
drug relies upon concomitant use of Cremophor EL (polyoxyl 35 castor oil, USP/NF) to produce an
adequately soluble formulation. Unfortunately, Cremophor EL use is also associated with patient toxicity
as it is not well tolerated and leads to hypersensitivity reactions in some individuals.
To overcome these difficulties, clinicians have attempted to prolong infusion schedules or use
corticosteroids and anti-histamines as a part of a premedication regimen.
However, to improve the efficacy of paclitaxel in anti-cancer therapy, a potential solution must involve
reformulation of the drug into better-tolerated drug delivery vehicles.
Genexol-PM (Paclitaxel loaded polymeric micelle) parenteral formulation consists of spherical, polymeric
micelles, which do not aggregate or are taken-up by reticulo-endothelial system (RES) and thus freely
circulate throughout the vasculature. The need for using a cosolvent to solubilize a compound is
eliminated, thereby reducing the overall toxicity of the formulation. Reducing overall toxicity potentially
enables higher dose administration, which could improve therapeutic response. Eliminating the use of
a cosolvent also eliminates any risk that the compound will precipitate in situ upon contact with blood,
which again improves the safety profile for this drug. Some cosolvents require special administration
sets to eliminate the risk of leaching plasticizer during infusion. Paclitaxel loaded polymeric micelle
formulations does not require special infusion sets.
Genexol-PM is undergoing phase II human clinical investigation in USA in a selected cancer. The Korean
development of Genexol-PM is progressing rapidly and three Phase II clinical studies in breast and
lung cancers are expected to conclude within year 2005 with the hope product launch in year 2006.
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| Features |
 Cremophor EL Free Formulation Of Paclitaxel : Free From Toxic Surfactants
Easy To Reconstitute Sterile Lyophilized Formulation
Fast Blood Clearance
High MTD Confirmed
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| Advantages |
Low Adverse Reaction Rate Expected
High Intratumor Concentration Of Paclitaxel Observed (Animal Studies)
Pre-Medication May Not Be Required in All Patients
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| Benefits |
High Therapeutic Response
High Safety Profile
Low Growth Factor Rescue
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Samyang's PM platform is a non-toxic, biodegradable polymer based system
for solubilization of poorly
soluble drugs |
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Patented biodegradable di-block copolymer composed of
methoxy poly(ethylene glycol)-poly
(lactide) [mPEG-PLA]
Core(Hydrophobic)-shell(Hydrophilic) structure
High solubilizing power for hydrophobic drugs
Self-forming polymeric micelles of nanometer size (ca., 10 ~ 200nm)
Apparent thermodynamic stability (i.e., low CMC)
In Vivo Anti-tumor Efficacy |
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