# US 7,745,408 B2 · Method of inducing melanogenesis in humans with MC1R variant alleles

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- Number: US 7,745,408 B2
- Document ID: US7745408B2
- Status: Granted
- Kind: B2
- Application number: 10/595,971
- Filed: 2004-11-23
- Published: 2008-01-03
- Granted: 2010-06-29
- Earliest claimed: 2003-11-24
- Assignees: Clinuvel Pharmaceuticals Limited
- Inventors: Stuart Michael Humphrey
- Web page: https://patentgrep.com/patent/US7745408B2

## CPC

- A61K 38/34: Melanocyte stimulating hormone [MSH], e.g. alpha- or beta-melanotropin
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/16: Emollients or protectives, e.g. against radiation
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/04: for chemically tanning the skin (topical sun or radiation screening or tanning preparations A61Q17/04)
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

A method for inducing melanogenesis in a human subject having a melanocortin 1 receptor (MC1R) variant allele associated with loss of or diminished receptor function comprises administering to said subject an amount of an α-melanocyte stimulating hormone (α-MSH) analogue effective to induce melanogenesis by the melanocytes in the skin or other epidermal tissue of the subject.

## Claims

### Claim 1

A method for inducing melanogenesis in a human subject having a melanocortin 1 receptor (MC1R) variant allele associated with loss of or diminished receptor function, which comprises the steps of:
i) identifying the MC1R variant using primer sequences selected from 5′-tggacaggactatggctgtg-3′ (MC1R-1F—SEQ ID NO:1), 5′-tcttcagcacgctcttcat-3′ (MC1R-1R—SEQ ID NO:2), 5′cttctacgcactgcgctacc-3′ (MC1R-2F—SEQ ID NO: 3) and 5′-gctttaagtgtgctgggcag-3′ (MC1R-2R—SEQ ID NO: 4), and
ii) administering to said subject an amount of [Nle4, DPhe7]-α-melanocyte stimulating hormone ([Nle4, DPhe7]-α-MSH) effective to induce melanogenesis by the melanocytes in the skin or other epidermal tissue of the subject.

### Claim 2 (depends on 1)

The method of claim 1, wherein an admixture of said [Nle4, DPhe7]-α-MSH with a further α-MSH analogue is administered in an amount effective to induce said melanogenesis, wherein said further α-MSH analogue is selected from:
(a) compounds of the formula:
Ac-Ser-Tyr-Ser-M-Gln-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2
wherein M is Met, Nle or Lys; and
(b) compounds of the formula:
R1—W—X—Y—Z—R2
wherein
R1 is Ac-Gly-, Ac-Met-Glu, Ac-Nle-Glu-, or Ac-Tyr-Glu-;
W is -His- or -D-His-;
X is -Phe-, -D-Phe-, -Tyr-, -D-Tyr-, or -(pNO2)D-Phe7-;
Y is -Arg- or -D-Arg-;
Z is -Trp- or -D-Trp-; and
R2 is -NH2; -Gly-NH2; or -Gly-Lys-NH2.

### Claim 3 (depends on 1)

The method of claim 1, wherein an admixture of said [Nle4, DPhe7]-α-MSH with a further α-MSH analogue is administered in an amount effective to induce said melanogenesis, wherein the further α-MSH analogue is selected from the group consisting of:
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Lys-Gly-Pro-Val-NH2,
Ac-Ser-Tyr-Ser-Nle-Asp-His-D-Phe-Arg-Trp-Lys-Gly-Pro-Val-NH2,
Ac-Nle-Glu-His-D-Phe-Arg-Trp-Lys-Gly-Pro-Val-NH2,
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys-Gly-Pro-Val-NH2,
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Gly-NH2,
Ac-Nle-Glu-His-D-Phe-Arg-Trp-Lys-NH2,
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys-NH2,
Ac-Nle-Glu-His-D-Phe-Arg-Trp-Orn-NH2,
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Orn-NH2,
Ac-Nle-Glu-His-D-Phe-Arg-Trp-Dab-NH2,
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Dab-NH2,
Ac-Nle-Glu-His-D-Phe-Arg-Trp-Dpr-NH2,
Ac-Nle-Glu-His-Phe-Arg-Trp-Lys-NH2 (SEQ ID NO:5)
, and
Ac-Nle-Asp-His-Phe-Arg-Trp-Lys-NH2 (SEQ ID NO:6)
.

### Claim 4 (depends on 1)

The method of claim 1, wherein an admixture of said [Nle4, DPhe7]-α-MSH with a further α-MSH analogue is administered in an amount effective to induce said melanogenesis wherein the further α-MSH analogue is selected from the group consisting of:

### Claim 5 (depends on 1)

The method of claim 1, wherein an admixture of said [Nle4, DPhe7]-α-MSH with a further α-MSH analogue is administered in an amount effective to induce said melanogenesis wherein the further α-MSH analogue is:

### Claim 6 (depends on 1)

The method of claim 1, wherein an admixture of said [Nle4, DPhe7]-α-MSH with a further α-MSH analogue is administered in an amount effective to induce said melanogenesis wherein the further α-MSH analogue is:
[Nle4,D-Phe7]-α-MSH4-10,
[Nle4,D-Phe7]-α-MSH4-11,
[Nle4,D-Phe7]-α-MSH4-11, or
[Nle4,D-Phe7]-α-MSH4-9.

### Claim 7 (depends on 1)

A method according to claim 1 wherein the human subject has one or more variant alleles selected from the group consisting of Val60Leu (V60L), Asp84Glu (D84E), Va192Met (V92M), Arg142His (R142H), Arg 151Cys (R151C), Arg160Trp (R160W), and Asp294His (D294H).

### Claim 8 (depends on 1)

A method according to claim 1 wherein the human subject has two or more variant alleles selected from the group consisting of Val60Leu (V60L), Asp84Glu (D84E), Va192Met (V92M), Arg142His (R142H), Arg 151Cys (R151C), Arg160Trp (R160W), and Asp294His (D294H).

### Claim 9 (depends on 1)

A method according to claim 1 wherein the human subject has a Fitzpatrick skin type of I or II.