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Camptothecin-peptide conjugates and pharmaceutical compositions containing the same

A composition and conjugate technology, applied in the field of new compounds, can solve problems such as insufficient intracellular delivery

Inactive Publication Date: 2013-04-10
德莱斯医药公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These studies show that the half-life (stability) of the conjugate is less than three minutes, which appears to be insufficient for intracellular delivery of therapeutically effective amounts of camptothecin derivatives in vivo

Method used

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  • Camptothecin-peptide conjugates and pharmaceutical compositions containing the same
  • Camptothecin-peptide conjugates and pharmaceutical compositions containing the same
  • Camptothecin-peptide conjugates and pharmaceutical compositions containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0226] I. Materials and methods

[0227] I.1a Cell Penetrating Peptide (CPP)

[0228] DPV3: Arg Lys Lys Arg Arg Arg Glu Ser Arg Lys Lys Arg Arg Arg Glu Ser (SEQ ID NO.1)

[0229] DPV1047: Val Lys Arg Gly Leu Lys Leu Arg His Val Arg Pro Arg Val Thr Arg Met Asp Val (SEQ ID NO.8)

[0230] DPV15: Leu Arg Arg Glu Arg Gln Ser Arg Leu Arg Arg Glu Arg Gln Ser Arg (SEQ ID NO.10)

[0231] DPV15b: Gly Ala Tyr Asp Leu Arg Arg Arg Glu Arg Gln Ser Arg Leu Arg Arg Arg Arg Glu ArgGln Ser Arg (SEQ ID NO.11)

[0232] DPV7: Gly Lys Arg Lys Lys Lys Lys Gly Lys Leu Gly Lys Lys Lys Arg Asp Pro (SEQ ID NO.3)

[0233] Tat 48-60 : Gly Arg Lys Lys Arg Arg Gln Arg Arg Arg Pro Pro Gln (SEQ ID NO.44)

[0234] Penetrating peptide: Arg Gln Ile Lys Ile Trp Phe Gln Asn Arg Arg Met Lys Trp Lys Lys (SEQ ID NO.29)

[0235] DPV51 (D) : D-Lys D-Arg Gly D-Leu D-Lys D-Leu D-Arg D-His (SEQ ID NO.51)

[0236] DPV1047 (D) : Val Lys Arg Gly Leu Lys Leu Arg His Val Arg Pro Arg Val Thr Arg Met AspVal (SEQ ID ...

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Abstract

The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptidic moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.

Description

[0001] The present invention relates to a novel compound for use in improved delivery of a therapeutic agent to a target cell or tissue, compositions comprising it and uses thereof. Said compounds are more particularly conjugates of peptide moieties and camptothecin, derivatives or analogs thereof, which provide a number of benefits including improved water solubility, pharmacokinetics and tissue distribution, increased therapeutic index, and Limitation of metabolic variability in patients and improved delivery of bioactive ingredients to target cells or tissues. Background of the invention [0002] Camptothecin (CPT) is an alkaloid extracted from Camtpotheca acuminata discovered in the 1960s (Wall et al., J. Amer. Chem. Soc. 88:3888-3890 (1966)). This water-insoluble molecule shows very strong antitumor activity, but its clinical application is limited due to strong bladder toxicity and severe diarrhea (Gottlieb et al., Cancer Chemother.Rep.54: 461-470 (1970 ), Moertel et al...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/66
CPCA61K47/48246A61K47/48338A61K47/64A61K47/65
Inventor M·米歇尔D·拉威尔F·里布I·特郎尚
Owner 德莱斯医药公司
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