# US 10,117,956 B2 · Radiolabeled active targeting pharmaceutical composition and the use thereof

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- Number: US 10,117,956 B2
- Document ID: US10117956B2
- Status: Granted
- Kind: B2
- Application number: 15/704,378
- Filed: 2017-09-14
- Published: 2018-05-03
- Granted: 2018-11-06
- Earliest claimed: 2013-09-18
- Assignees: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan
- Applicants: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan
- Inventors: Hsin-Ell Wang; Chien-Chung Hsia; Mao-Chi Weng; Kun-Liang Lin; Hao-Wen Kao; Chao-Cheng Chen; Kwan-Hwa Chi; Der-Chi Tien; Wuu-Jyh Lin
- Web page: https://patentgrep.com/patent/US10117956B2

## CPC

- A61K 51/1093: {conjugates with carriers being antibodies}
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61K 51/103: {against receptors for growth factors or receptors for growth regulators}
- A61K 51/1244: {microparticles or nanoparticles, e.g. polymeric nanoparticles}
- A61P 35/00: Antineoplastic agents
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention is related to a radiolabeled active targeting pharmaceutical composition, including: a bioconjugate and a radionuclide, wherein the bioconjugate includes a biomolecule and a metal nanoparticle, wherein the biomolecule has an affinity for receptors on the surface of a cell membrane and is selected from the group consisting of a peptide and a protein. The present invention further provides a method for evaluating a thermal adjuvant therapy for tumors and a kit thereof. The above-mentioned pharmaceutical composition is applied to evaluate a tumor accumulation time, so as to establish the optimal policy for a radiofrequency- or laser-induced thermal adjuvant therapy for tumors.

## Claims

### Claim 1

A radiolabeled active targeting pharmaceutical composition, comprising:
a bioconjugate, comprising a peptide, a metal nanoparticle, and an intercalating agent, wherein the peptide is a Bombesin (BBN) peptide combined with maleimido-lipoamide, the intercalating agent is diethylene triamine pentaacetic acid (DTPA), and the metal nanoparticle is Au nanoparticle; and
a radionuclide, selected from the group consisting of: indium, iodine, lutetium, rhenium, gallium, and yttrium.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the metal nanoparticle further has a thiol group through surface modification.