# US 4,397,843 A · Mannose-6-phosphate-low density protein reagent effective against hypercholesterolemia

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- Number: US 4,397,843 A
- Document ID: US4397843A
- Status: Granted
- Kind: A
- Application number: 06/341,572
- Filed: 1982-01-21
- Granted: 1983-08-09
- Earliest claimed: 1980-10-23
- Assignees: The United States of America as represented by the Department of Health and Human Services
- Inventors: David M. Neville, Jr.; Richard J. Youle; Gary J. Murray
- Web page: https://patentgrep.com/patent/US4397843A

## CPC

- C07K 14/415: from plants
- A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof
- A61K 47/6823: {Double chain ricin}
- C07K 14/775: Apolipopeptides
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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)

## Abstract

A new reagent effective in inhibiting cholesterol synthesis 75% in human fibroblasts derived from patients suffering from the disease familial hypercholestrolemia is Man6P-low density lipoprotein and is effective in tissue culture test systems at 100 .mu.g/ml after a ten-hour exposure. The broad purpose of this invention is to modify the receptor specificity of a protein so that it will enter cells which were previously impermeable and exert new effects or reverse a pathological condition. That is, the compound of this invention is a useful reagent in the selective cytotoxic treatment of hypercholesterolemia.

## Claims

### Claim 1

A reagent for treating familial hypercholestrolemia comprising an effective amount of mannose-6-phosphate-low density lipoprotein.

### Claim 2

A cholesterol synthesis inhibiting reagent composition comprising an effective amount of mannose-6-phosphate-low density protein.