FORMULATIONS OF GROWTH HORMONE RELEASING FACTOR (GRF) MOLECULES WITH IMPROVED STABILITY
    1.
    发明公开

    公开(公告)号:EP2961432A1

    公开(公告)日:2016-01-06

    申请号:EP14756414.0

    申请日:2014-02-26

    IPC分类号: A61K47/40 A61K38/25 A61K9/19

    摘要: Stabilized solid and liquid pharmaceutical formulations comprising a GRF molecule as active ingredient, such as GRF analogs including those comprising an N-terminal-attached hydrophobic moiety, such as [trans-3-hexenoyl]hGHRH (1-44) amide, are disclosed. The formulation comprises a GRF molecule or a pharmaceutically acceptable salt thereof and a β- cyclodextrin which is not conjugated to the GRF molecule or salt thereof. Also disclosed is the use of the formulation for the treatment of various conditions, methods of preparing the formulation, as well as kits containing it. Methods of stabilizing (e.g., with respect to chemical stability) such GRF molecules, as well as methods of inhibiting their deamidation at Asn
    8 , are also disclosed.

    USE OF (HEXENOYL TRANS-3)HGRF(1-44)NH2 AND RITONAVIR IN COMBINATION THERAPY
    3.
    发明公开
    USE OF (HEXENOYL TRANS-3)HGRF(1-44)NH2 AND RITONAVIR IN COMBINATION THERAPY 审中-公开
    使用(己烯酰TRANS-3)的hGRF(1-44)NH 2和利托那韦在组合疗法

    公开(公告)号:EP2421547A1

    公开(公告)日:2012-02-29

    申请号:EP10766537.4

    申请日:2010-04-20

    摘要: A combination therapy is described comprising the protease inhibitor Ritonavir and the growth hormone releasing factor (GRF) analogue (hexenoyl trans-3)hGRF(1-44)NH
    2 (TH9507), for the treatment of HIV- associated lipodystrophy. Human growth hormone may modulate cytochrome P450 (CYP) enzyme activity. Therefore, the potential impact of tesamorelin on CYP3A activity was investigated by examining its effect on the pharmacokinetics (PK) of ritonavir (a CYP3 A-inhibitor), a drug that is potentially administered concomitantly with tesamorelin. This study showed that the impact of tesamorelin on CYP3A activity appears to be minimal. Ritonavir may be co-administered with tesamorelin, without changing the dosing regimen.

    USE OF (HEXENOYL TRANS-3)HGRF(L-44)NH2 AND SIMVASTATIN IN COMBINATION THERAPY
    8.
    发明公开
    USE OF (HEXENOYL TRANS-3)HGRF(L-44)NH2 AND SIMVASTATIN IN COMBINATION THERAPY 审中-公开
    使用(己烯酰反式-3)hGRF(L-44)NH 2和辛伐他汀在联合治疗

    公开(公告)号:EP2421548A1

    公开(公告)日:2012-02-29

    申请号:EP10766538.2

    申请日:2010-04-20

    摘要: A combination therapy is described comprising the CYP-metabolized compound Simvastatin and the growth hormone releasing factor (GRF) analogue (hexenoyl trans-3)hGRF(l-44)NH2 (tesamorelin), for the treatment of HIV- associated lipodystrophy. Human growth hormone may modulate cytochrome P450 (CYP) enzyme activity. Therefore, the potential impact of tesamorelin on CYP3A activity was investigated by examining its effect on the pharmacokinetics (PK) of simvastatin ( a CYP3A-substrate), a drug that is potentially administered concomitantly with tesamorelin. This study showed that the impact of tesamorelin on CYP3 A activity appears to be minimal. Simvastatin may be co-administered with tesamorelin, without changing the dosing regimen.

    GH SECRETAGOGUES AND USES THEREOF
    9.
    发明公开
    GH SECRETAGOGUES AND USES THEREOF 审中-公开
    GH分泌及其用途

    公开(公告)号:EP1812048A1

    公开(公告)日:2007-08-01

    申请号:EP05797145.9

    申请日:2005-10-20

    IPC分类号: A61K38/25 A61P37/00 A61P3/00

    CPC分类号: A61K38/27

    摘要: The invention relates to use of a GH secretagogue (e.g. GRF or an analog thereof) for (1) altering a lipid parameter in a subject; (2) altering a body composition parameter in a subject, (3) treating a condition characterized by deficient or decreased bone formation in a subject (4) improving daytime vigilance and/or cognitive function in a subject, (5) improving a metabolic condition in a subject, (6) improving anabolism in a catabolic condition in a subject, and/or (7) improving and/or reconstituting immune function in a subject.