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Targeted conjugates and particles and formulations thereof

A technology of conjugates and particles, which is applied in the field of molecules targeting somatostatin receptors in the treatment of cancer, can solve the problems of reducing treatment frequency and drug retention

Inactive Publication Date: 2018-02-16
TARVEDA THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the targeting of the delivery system may preferentially deliver the drug into the site where therapy is desired, the drug released from the nanoparticles may not be retained, for example, in effective amounts in the area of ​​the targeted cell, or may not be maintained in a relatively free manner. The toxic state remains in circulation for a sufficient amount of time to reduce the frequency of treatment or to allow lower amounts of drug to be administered while still achieving a therapeutic effect

Method used

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  • Targeted conjugates and particles and formulations thereof
  • Targeted conjugates and particles and formulations thereof
  • Targeted conjugates and particles and formulations thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0340] Formulations of the pharmaceutical compositions described herein can be prepared by any method known or hereafter developed in the art of pharmacology. In general, such preparation methods comprise the steps of bringing into association the active ingredient with excipients and / or one or more other auxiliary ingredients, followed by, if necessary and / or desired, dividing, shaping and / or Packaged in the desired single-dose or multi-dose units.

[0341] The pharmaceutical compositions of the present invention may be prepared, packaged and / or sold in bulk in single unit dosage form and / or in multiple single unit dosage forms. As used herein, a "unit dose" is an individual quantity of a pharmaceutical composition containing a predetermined quantity of an active ingredient. The amount of active ingredient is usually equal to the dose of active ingredient to be administered to the subject, and / or a suitable fraction of such a dose, such as, for example, one half or one third...

Embodiment A

[0489] Example A: HPLC Analysis Method: Product Analysis by C18 Reversed Phase HPLC (Method 1)

[0490]The compounds described herein were analyzed by HPLC on a Zorbax Eclipse XDB-C18 reverse phase column (4.6x 100mm, 3.5μm, Agilent PN: 961967-902), where the mobile phase consisted of water + 0.1% TFA (solvent A) and acetonitrile +0.1% TFA (solvent B) composition, flow rate was 1.5 mL / min, and column temperature was 35°C. The injection volume was 10 μL and the analytes were detected using UV at 220 and 254 nm. Gradients are shown in Table 3.

[0491] Table 3: Gradients

[0492] time (minutes)

Embodiment B

[0493] Example B: Control Compound

[0494] Non-activated compounds are designed with significant impairment of somatostatin receptor binding. The Lys residues of the Tyr-DTrp-Lys-Thr motif of the control compound were blocked such that the control compound did not have strong binding to the somatostatin receptor. Examples of control compounds include:

[0495]

[0496]

[0497]

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Abstract

Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as maytansinoid attached to a targeting moiety, such as a somatostatin receptorbinding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and / or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided.

Description

[0001] References to related applications [0002] This application claims priority to U.S. Provisional Patent Application No. 62 / 186,657, filed June 30, 2015, entitled Targeted Conjugates and Particles and Formulations Thereof, the contents of which are incorporated by reference in their entirety into this article. field of invention [0003] The present invention relates generally to the field of targeting ligands, conjugates thereof and particles comprising the conjugates. More specifically, the invention relates to the use of molecules targeting somatostatin receptors, for example for the treatment of cancer. Background of the invention [0004] Developments in nanomedicine often involve improving the pharmaceutical properties of drugs and, in some cases, enhancing targeted delivery in a more cell-specific manner. Several cell-specific drugs have been described and include monoclonal antibodies, aptamers, peptides and small molecules. Despite some potential advantages...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14
CPCA61K47/6929A61K47/64A61P35/00A61K31/5365A61K38/31A61K47/6937
Inventor B·H·怀特M·T·比洛多B·莫罗R·R·欣德P·林苏B·斯韦伊达-克拉维茨P·R·巴奇内R·G·阿拉戈瓦C·A·邓巴
Owner TARVEDA THERAPEUTICS INC
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