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US 2009/0258017 A1Published application
Lyophilized therapeutic peptibody Formulations
AssigneeAmgen Inc.
InventorsWilliam J. Callahan, Richard L. Remmele, JR., Gayathri Ratnaswamy, Ramil F. Latypov, Dingjiang Liu
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Abstract
The present invention provides long-term stable formulations of a lyophilized therapeutic peptibody and methods for making a lyophilized composition comprising a therapeutic peptibody.
Claims99
A lyophilized therapeutic peptibody composition comprising a buffer, a bulking agent, a stabilizing agent, and optionally a surfactant;
- wherein said buffer is comprised of a pH buffering agent in a range of about 5 mM to about 20 mM and wherein the pH is in a range of about 3.0 to about 8.0;
- wherein said bulking agent is at a concentration of about 0% to about 4.5% w/v;
- wherein said stabilizing agent is at a concentration of about 0.1% to about 20% w/v;
- wherein said surfactant is at a concentration of about 0.004% to about 0.4% w/v;
- and
- wherein said therapeutic peptibody comprises a structure set out in Formula I,
- [(X1)a—F1—(X2)b]-(L1)c-WSPd Formula I
- wherein:
- F1 is an Fc domain;
- X1 is selected from
- P1-(L2)e
- P2-(L3)f-P1-(L2)e—
- P3-(L4)g-P2-(L3)f-P1-(L2)e- and
- P4-(L5)h-P3-(L4)g-P2-(L3)-P1-(L2)e-
- X2 is selected from:
- -(L2)e-P1,
- -(L2)e-P1-(L3)f-P2,
- -(L2)e-P1-(L3)f-P2-(L4)g-P3, and
- -(L2)g-P1-(L3)f-P2-(L4)g-P3-(L5)h-P4
- wherein P1, P2, P3, and P4 are each independently sequences of pharmacologically active peptides;
- L1, L2, L3, L4, and L5 are each independently linkers;
- a, b, c, e, f, g, and h are each independently 0 or 1,
- provided that at least one of a and b is 1;
- d is 0, 1, or greater than 1;
- and
- WSP is a water soluble polymer, the attachment of which is effected at any reactive moiety in F1.
23 more elements
A method for making a lyophilized therapeutic peptibody comprising the steps of:
- a) preparing a solution of a buffer, a bulking agent, a stabilizing agent, and optionally a surfactant;
- wherein said buffer is comprised of a pH buffering agent in a range of about 5 mM to about 20 mM and wherein the pH is in a range of about 3.0 to about 8.0;
- wherein said bulking agent is at a concentration of about 2.5% to about 4% w/v;
- wherein said stabilizing agent is at a concentration of about 0.1% to about 5% w/v;
- wherein said surfactant is at a concentration of about 0.004% to about 0.04% w/v;
- and
- b) lyophilizing said therapeutic peptibody;
- wherein said therapeutic peptibody comprises a structure set out in Formula I,
- [(X1)a—F1—(X2)b]-(L1)c-WSPd Formula I
- wherein:
- F1 is an Fc domain;
- X1 is selected from
- P1-(L2)e—
- P2-(L3)f-P1-(L2)e—
- P3-(L4)g-P2-(L3)f-P1-(L2)e- and
- P4 (L5)h-P3-(L4)g-P2-(L3)f-P1-(L2)e—
- X2 is selected from:
- -(L2)e-P1,
- -(L2)e-P1-(L3)f-P2,
- -(L2)—P1-(L3)f-P2-(L4)g-P3, and
- -(L2)e-P1-(L3)f-P2-(L4)g P3-(L5)h-P4
- wherein P1, P2, P3, and P4 are each independently sequences of pharmacologically active peptides;
- L1, L1, L3, L4, and L are each independently linkers;
- a, b, c, e, f, g, and h are each independently 0 or 1,
- provided that at least one of a and b is 1;
- d is 0, 1, or greater than 1;
- and
- WSP is a water soluble polymer, the attachment of which is effected at any reactive moiety in F1.
25 more elements
Dependencies are inferred from the claim text.