# US 2021/0330659 A1 · Use of nicotinamide composition in preparation of drug for treating hand-foot skin reaction induced by sorafenib

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- Number: US 2021/0330659 A1
- Document ID: US20210330659A1
- Status: Published application
- Kind: A1
- Application number: 16/612,770
- Filed: 2018-10-31
- Published: 2021-10-28
- Earliest claimed: 2018-08-07
- Assignees: Zhejiang University
- Applicants: Zhejiang University
- Inventors: Qiaojun HE; Bo YANG; Peihua LUO
- Web page: https://patentgrep.com/patent/US20210330659A1

## CPC

- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61P 17/00: Drugs for dermatological disorders
- 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 disclosure provides a use of a nicotinamide composition in preparation of a drug for treating hand-foot skin reaction (HFSR) induced by sorafenib, the composition being consisted of nicotinamide and sorafenib in a dosage ratio of 2:3. The composition provided by the present disclosure can alleviate the HFSR caused by excessive keratinization induced by sorafenib. This protective effect is achieved by inhibiting HB-EGF/SIRT1 pathway. The present disclosure provides a mechanism of sorafenib-induced HFSR, i.e., the excessive activation of the HB-EGF/SIRT1 pathway, thereby providing a theoretical foundation for clinical research of sorafenib-induced HFSR. The present disclosure also provides a drug that can effectively treat sorafenib-induced HFSR, thereby greatly broadening the clinical application of sorafenib. Nicotinamide is highly clinically feasible due to its moderate price, and thus can be prepared in any suitable formulation according to the requirements.

## Claims

### Claim 1

A use of a nicotinamide composition in preparation of a drug for treating hand-foot skin reaction induced by sorafenib, wherein the composition consists of nicotinamide and sorafenib,
where in nicotinamide has a chemical name of 3-pyridinecarboxamide, a molecular formula of C6H6N2O, and a molecular weight of 122.13, and
sorafenib has a chemical name of 4-{4-[({4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine -2-carboxamide, a molecular formula of C21H16ClF3N4O3, and a molecular weight of 464.83.

### Claim 2 (depends on 1)

The use of a nicotinamide composition in preparation of a drug for treating hand-foot skin reaction induced by sorafenib according to claim 1, wherein in the composition, a dosage ratio of nicotinamide to sorafenib is 2:3.

### Claim 3 (depends on 1)

The use of a nicotinamide composition in preparation of a drug for treating hand-foot skin reaction induced by sorafenib according to claim 1, wherein the drug is prepared with a composition of nicotinamide and sorafenib and a pharmaceutically acceptable adjuvant, and the drug is in a liquid formulation or a solid formulation.