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New therapy and medicament using integrin ligands for treating cancer

A technology of integrin and ligand, which is applied in the direction of drug combination, peptide/protein composition, medical preparations containing active ingredients, etc., can solve the problem of reducing curative effect

Inactive Publication Date: 2011-10-19
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many physiological barriers and pharmacokinetic parameters have the effect of reducing its efficacy

Method used

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  • New therapy and medicament using integrin ligands for treating cancer
  • New therapy and medicament using integrin ligands for treating cancer
  • New therapy and medicament using integrin ligands for treating cancer

Examples

Experimental program
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example

[0589] The following flow chart describes an example of a method of treatment comprising application of whole brain radiation and administration of cyclo-(Arg-Gly-Asp-DPhe-NMeVal) and / or a pharmaceutically acceptable salt thereof, preferably cyclo-(Arg-Gly- Asp-DPhe-NMeVal) (= Cilengitide):

[0590]

[0591] The following flow chart describes an example of a study design for a therapeutic approach consisting of application of whole brain radiation and administration of cyclic-(Arg-Gly-Asp-DPhe-NMeVal) and / or a pharmaceutically acceptable salt thereof, preferably cyclic-(Arg -Gly-Asp-DPhe-NMeVal) (= Cilengitide) composition:

[0592]

[0593] Particularly preferred subjects of the invention are all uses, methods of treatment, medicaments, individuals of the invention, embodiments of the invention and / or methods of preparation described herein

[0594] i) It comprises the administration of at least one specific integrin ligand in one or more doses such that the weekly dos...

Embodiment 1

[1138] Example 1: Radiotherapy, Cilengitide (= Cyclo-(Arg-Gly-Asp-DPhe-Nme-Val)) Timing Experiment in a Rat Orthotopic Glioblastoma Model

[1139] NIH rnu nude rats were anesthetized, bound, and injected intracerebrally with 5×10E5U251 human glioblastoma cells suspended in 10 μL of cell culture medium at a depth of 1 mm behind the orbit, 3 mm and 2.5 mm to the right of the anterior blemish, A #2701 Hamilton syringe fitted with a 26-gauge needle was used, and injections were performed essentially as previously described (Engebraaten et al., 1999). 14 days later, at various times prior to monotherapy with application of a single, parallel, dorsal-ventral 6MV x-ray beam so that 95-100% of the central axis dose of 25 Gy hits the tumor volume (Kim et al., 1999) (8h, 4h, 2h, 1h), Cilengitide (4 mg / kg) in PBS was administered as an intraperitoneal bolus. Animals also received the same intraperitoneal bolus of cilengitide each day for the next 7 days. Animals were maintained under c...

Embodiment 2

[1153] Example 2: Phase IIa trial of cilengitide ((=cyclo-(Arg-Gly-Asp-DPhe-NMe-Val)) single agent therapy in patients with recurrent glioblastoma

[1154] Background: This phase IIa study was designed to evaluate the cyclic RGD pentapeptide cilengitide ((=cyclo-(Arg-Gly-Asp-DPhe-NMe-Val), an inhibitor of integrins avβ3 and avβ5) as a single active agent , safety, toxicity and clinical activity in patients (pts) with relapsed glioblastoma (GBM) at doses of 500 mg and 2000 mg.

[1155]METHODS: In this multicentre, open-label, randomized, and uncontrolled study, pts with recurrent GBM and detectable disease following previous treatment with temozolomide and radiation therapy were randomized to receive a dose of 500 mg Or 2000mg of cilengitide intravenously twice a week until disease progression. Independent blinded examinations were performed for histopathological diagnosis and MRI imaging. The primary endpoint was progression-free survival (PFS) at 6 months (mths). Secondary...

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Abstract

The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agents or therapy forms that have synergistic efficacy when administered consecutively with said ligands, such as chemotherapeutic agents and or radiation therapy. The therapy results in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone, concurrently or not in the dosage regime of the present invention.

Description

[0001] Technical field of invention: [0002] The present invention relates to specific therapeutic modalities for the treatment of tumors and tumor metastases comprising the administration of an integrin ligand and a cancer co-therapeutic agent or other cancer co-therapeutic modality when combined with said Integrin ligands that have an additive or synergistic effect when administered together, such as chemotherapeutics, immunotherapeutics (including antibodies), radioimmunoconjugates, and immune cell co-therapeutics, or other forms of cancer co-therapy Factor and / or radiation therapy is preferably administered in a timed manner. This treatment will result in a synergistic potential potentiation of the inhibitory effect of each individual treatment on tumor cell and tumor endothelial cell proliferation, resulting in a more effective treatment than when the individual components are administered alone, together or in other treatment regimens than the treatment regimens of the pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00A61K38/08A61K38/12A61K31/00
CPCA61K38/08A61K38/12A61K45/06A61N5/10A61P11/00A61P15/00A61P25/00A61P35/00A61P35/04A61P43/00A61K2300/00
Inventor M·A·皮卡德C·马内戈尔德H·惠勒M·哈斯劳B·内恩斯
Owner MERCK PATENT GMBH
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