JPWO2020007857A5 - - Google Patents

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Publication number
JPWO2020007857A5
JPWO2020007857A5 JP2020570554A JP2020570554A JPWO2020007857A5 JP WO2020007857 A5 JPWO2020007857 A5 JP WO2020007857A5 JP 2020570554 A JP2020570554 A JP 2020570554A JP 2020570554 A JP2020570554 A JP 2020570554A JP WO2020007857 A5 JPWO2020007857 A5 JP WO2020007857A5
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JP
Japan
Prior art keywords
teverelix
composition
tfa
trifluoroacetic acid
mol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Application number
JP2020570554A
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Japanese (ja)
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JP7181318B2 (en
JP2021529165A (en
Publication date
Priority claimed from EP18181945.9A external-priority patent/EP3590525A1/en
Application filed filed Critical
Publication of JP2021529165A publication Critical patent/JP2021529165A/en
Publication of JPWO2020007857A5 publication Critical patent/JPWO2020007857A5/ja
Priority to JP2022183797A priority Critical patent/JP2023027082A/en
Application granted granted Critical
Publication of JP7181318B2 publication Critical patent/JP7181318B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Claims (8)

少なくとも１：２．４、かつ１：２．８以下のテベレリクス（Ａｃ－Ｄ－Ｎａｌ－Ｄ－ｐＣｌＰｈｅ－Ｄ－Ｐａｌ－Ｓｅｒ－Ｔｙｒ－Ｄ－Ｈｃｉ－Ｌｅｕ－Ｌｙｓ（ｉＰｒ）－Ｐｒｏ－Ｄ－Ａｌａ－ＮＨ２）とトリフルオロアセテートとのモル比を有し、組成物中のテベレリクス１モルにつき、組成物が、少なくとも２．４ｍｏｌのトリフルオロアセテート、かつ２．８ｍｏｌ以下のトリフルオロアセテートを含み、前記組成物中の不溶型微結晶テベレリクスの量が、均一テベレリクス－ＴＦＡ組成物の重量を基準として、少なくとも８０重量％である、均一テベレリクス－ＴＦＡ組成物。 At least 1: 2.4 and 1: 2.8 or less Teverelix (Ac-D-Nal-D-pClPhe-D-Pal-Ser-Tyr-D-Hci-Leu-Lys (iPr) -Pro-D- It has a molar ratio of Ala-NH 2 ) to trifluoroacetic acid, and the composition is at least 2. It contains 4 mol of trifluoroacetic acid and 2.8 mol or less of trifluoroacetic acid, and the amount of insoluble microcrystalline Teverelix in the composition is at least 80% by weight based on the weight of the uniform Teverelix-TFA composition. A uniform Teverelix-TFA composition. 医薬として使用するための、請求項１に記載のテベレリクス－ＴＦＡ組成物。 The Teverelix-TFA composition according to claim 1 for use as a pharmaceutical. ゴナドトロピンホルモンの放出に関連する症状または疾患の治療に使用するためのテベレリクス－ＴＦＡ組成物であって、前記症状または疾患が、良性前立腺過形成；急性閉尿；子宮内膜症；前立腺がん、乳がん、もしくは子宮頸がんなどのがん；またはこれらの組み合わせである、請求項１または２に記載のテベレリクス－ＴＦＡ組成物。 A Teverelix-TFA composition for use in the treatment of symptoms or disorders associated with the release of gonadotropin hormone, wherein the symptoms or disorders are benign prostate hyperplasia; acute urinary closure; endometriosis; prostate cancer, The Teverelix-TFA composition according to claim 1 or 2 , which is a cancer such as breast cancer or cervical cancer; or a combination thereof. 請求項１から３のいずれか一項に記載のテベレリクス－ＴＦＡ組成物を含む、薬学的製剤。 A pharmaceutical preparation comprising the Teverelix-TFA composition according to any one of claims 1 to 3 . 微結晶均一水性懸濁液の形態であり、テベレリクスとトリフルオロアセテートとのモル比が１：２．４から１：２．８の間であり、組成物中のテベレリクス１モルにつき、組成物が、２．４から２．８ｍｏｌの間のトリフルオロアセテートを含む、請求項４に記載の薬学的製剤。 It is in the form of a polycrystalline uniform aqueous suspension, and the molar ratio of teverelix to trifluoroacetate is 1: 2. Between 4 and 1: 2.8, for every mole of Teverelix in the composition, the composition is 2. The pharmaceutical preparation according to claim 4 , which comprises trifluoroacetic acid between 4 and 2.8 mol. 請求項１から３のいずれか一項に記載のテベレリクス－ＴＦＡ組成物、または請求項４もしくは５に記載の薬学的製剤を充填した、包装。 A package filled with the Teverelix-TFA composition according to any one of claims 1 to 3 or the pharmaceutical preparation according to claim 4 or 5 . 単位投与量の、請求項１から３のいずれか一項に記載のテベレリクス－ＴＦＡ組成物、または請求項４もしくは５に記載の薬学的製剤を含む、請求項６に記載の包装。 The packaging of claim 6 , wherein the unit dose comprises the Teverelix-TFA composition of any one of claims 1 to 3 , or the pharmaceutical formulation of claim 4 or 5 . 包装が、皮下および／または筋肉内注射を提供するのに好適なシリンジである、請求項６または７に記載の包装。 The packaging according to claim 6 or 7 , wherein the packaging is a syringe suitable for providing subcutaneous and / or intramuscular injection.
JP2020570554A 2018-07-05 2019-07-02 Teverelix-TFA composition Active JP7181318B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2022183797A JP2023027082A (en) 2018-07-05 2022-11-17 Teverelix-TFA composition

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18181945.9 2018-07-05
EP18181945.9A EP3590525A1 (en) 2018-07-05 2018-07-05 Teverelix-tfa composition
PCT/EP2019/067728 WO2020007857A1 (en) 2018-07-05 2019-07-02 Teverelix-tfa composition

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2022183797A Division JP2023027082A (en) 2018-07-05 2022-11-17 Teverelix-TFA composition

Publications (3)

Publication Number Publication Date
JP2021529165A JP2021529165A (en) 2021-10-28
JPWO2020007857A5 true JPWO2020007857A5 (en) 2022-06-14
JP7181318B2 JP7181318B2 (en) 2022-11-30

Family

ID=62874669

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2020570554A Active JP7181318B2 (en) 2018-07-05 2019-07-02 Teverelix-TFA composition
JP2022183797A Pending JP2023027082A (en) 2018-07-05 2022-11-17 Teverelix-TFA composition

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2022183797A Pending JP2023027082A (en) 2018-07-05 2022-11-17 Teverelix-TFA composition

Country Status (6)

Country Link
US (2) US11357818B2 (en)
EP (3) EP3590525A1 (en)
JP (2) JP7181318B2 (en)
CN (1) CN112423775B (en)
CA (1) CA3141519A1 (en)
WO (1) WO2020007857A1 (en)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3985723A (en) * 1971-09-07 1976-10-12 The University Of Mississippi Trifluoroacetylation process
US7098305B2 (en) 2001-09-06 2006-08-29 Ardana Bioscience Limited Sustained release of microcrystalline peptide suspensions
EP1674082A1 (en) * 2004-12-22 2006-06-28 Zentaris GmbH Process for the manufacture of sterile suspensions or lyophilisates of low-soluble basic peptide complexes, pharmaceutical formulations comprising these complexes and their use as medicament
WO2008071984A1 (en) * 2006-12-13 2008-06-19 Ardana Bioscience Limited Administration of the gonadotropin-releasing hormone antagonist teverelix
CN105693844A (en) * 2016-03-10 2016-06-22 泰州施美康多肽药物技术有限公司 Preparation method of gonadotrophin-releasing hormone analogue acetate
EP3560555A1 (en) * 2018-04-26 2019-10-30 LifeArc A composition for treating one or more estrogen related diseases

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