CALCITONIN DRUG-OLIGOMER CONJUGATES, AND USES THEREOF

• US 20100105624A1
• Filed: 10/27/2009
• Published: 04/29/2010
• Est. Priority Date: 06/04/2001
• Status: Active Grant

• Current Assignee: Balasingam Radhakrishnan, Nnochiri N. Ekwuribe
• Original Assignee: Balasingam Radhakrishnan, Nnochiri N. Ekwuribe
• Inventors: Radhakrishnan, Balasingam, Ekwuribe, Nnochiri N.
• Granted Patent: US 8,030,269 B2
• Time in Patent Office: Days
• US Class Current: 514/1.100
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: C07K 14/585 Calcitonins

Abstract

Calcitonin drug-oligomer conjugates that include a calcitonin drug coupled to an oligomer including a single polyalkylene glycol moiety consisting of between 4 and 10 polyalkylene glycol subunits are disclosed. Pharmaceutical compositions including such conjugates and methods of treating bone disorders by administering such conjugates are also disclosed.

Claims

1. A monodispersed calcitonin-oligomer conjugate comprising salmon calcitonin coupled to two oligomer subunits, wherein each oligomer consists of the structure of Formula I:

and wherein the first oligomer subunit is covalently coupled to Lys¹¹ of said salmon calcitonin and the second oligomer is covalently coupled to Lys¹⁸ of said salmon calcitonin.

2. A pharmaceutical composition comprising the conjugate mixture of claim 1;

and a pharmaceutically acceptable carrier.

3. A method of treating a bone disorder in a subject in need of such treatment, said method comprising:

administering an effective amount of a calcitonin drug-oligomer conjugate according to claim 1 to the subject to treat the bone disorder.

4. The method according to claim 3, wherein administration is oral.