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Generated: September 22, 2017

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Title:Weakly acidic pH-responsive peptide and liposome containing same
Abstract: A problem to be solved by the present invention is to provide a peptide compound for producing a drug delivery carrier capable of releasing a target substance in a weakly acidic pH environment. The present invention provides a peptide compound comprising a hydrophilic amino acid block and a hydrophobic amino acid block; [1] the peptide compound containing 24 to 36 amino acids in total; [2] the hydrophilic amino acid block containing 4 to 10 amino acids in total and having an average hydropathy index of -3.0 to -1.0; and [3] the hydrophobic amino acid block containing 20 to 32 amino acids in total, containing one or more His residues, and having an average hydropathy index of 1.0 to 2.5.
Inventor(s): Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP)
Assignee: Taiho Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:14/430,723
Patent Claims:1. A peptide compound comprising a hydrophilic amino acid block and a hydrophobic amino acid block; [1] the peptide compound consisting of 24 to 36 amino acids in total; [2] the hydrophilic amino acid block consisting of 4 to 10 amino acids in total and having an average hydropathy index of -3.0 to -1.0; and [3] the hydrophobic amino acid block consisting of 20 to 32 amino acids in total, containing one or more His residues, and having an average hydropathy index of 1.0 to 2.5; wherein when the hydrophobic amino acid block comprises two or more amino acids having a hydropathy index of -3.0 or less, amino acids having a hydropathy index of -3.0 or less are not adjacent to each other in the hydrophobic amino acid block.

2. The peptide compound according to claim 1, wherein the hydrophilic amino acid block has an average hydropathy index of -2.0 to -1.5; and the hydrophobic amino acid block has an average hydropathy index of 1.5 to 2.0.

3. The peptide compound according to claim 1, wherein the hydrophilic amino acid block comprises an amino acid having a hydropathy index of -3.0 or less and an amino acid having a hydropathy index of 0 to -1.0; and the hydrophobic amino acid block comprises His and an amino acid having a hydropathy index of higher than 0.

4. The peptide compound according to claim 1, wherein the amino acids constituting the hydrophilic amino acid block are His or Glu, and Gly; and the amino acids constituting the hydrophobic amino acid block are His and any amino acid selected from the group consisting of Leu, Ala, Met, Cys, Phe, Val, and Ile.

5. The peptide compound according to claim 1, wherein the hydrophilic amino acid block has a peptide sequence containing 0 to 5 His residues; and the hydrophobic amino acid block has a peptide sequence containing 1 to 8 His residues.

6. The peptide compound according to claim 1, wherein the hydrophilic amino acid block is represented by the following formula (I): (AA.sub.1)(AA.sub.2)(AA.sub.3)(AA.sub.4) (I) wherein any two of AA.sub.1, AA.sub.2, AA.sub.3, and AA.sub.4 are His or Glu, and the other two are Gly; and the hydrophobic amino acid block contains 5 to 8 units represented by the following formula (II): (AA.sub.5)(AA.sub.6)(AA.sub.7)(AA.sub.8) (II) wherein AA.sub.5, AA.sub.6, AA.sub.7, and AA.sub.8 are the same or different, and each represents His, Leu, or Ala, with the proviso that at least one of the units of the formula (II) contains one or two His residues; each unit may have the same or different amino acid sequence.

7. A liposome comprising the peptide compound according to claim 1, and a lipid.

8. The liposome according to claim 7, wherein the liposome comprises 1 to 10 mol % of the peptide compound based on the total amount of lipids in the liposome.

9. The liposome according to claim 8, wherein the liposome is a cationic liposome.

10. The liposome according to claim 7, wherein the liposome encapsulates a target substance.

11. A pharmaceutical composition comprising the liposome according to claim 10, in combination with a pharmaceutically acceptable carrier, wherein said target substance is selected from the group consisting of drugs, nucleic acids, peptides, and proteins.

12. An antitumor agent comprising the liposome according to claim 10, wherein said target substance is an anticancer agent.

13. The antitumor agent according to claim 12, wherein said cancer agent is selected from the group consisting of tegafur, doxorubicin, daunorubicin, cis-platinum, oxaliplatin, carboplatin, paclitaxel, irinotecan, SN-38, actinomycin D, vincristine, vinblastine, methotrexate, fluorouracil, mitomycin C, docetaxel, cyclophosphamide, capecitabine, epirubicin, gemcitabine, mitoxantrone, leucovorin, vinorelbine, trastuzumab, etoposide, estramustine, prednisone, interferon .alpha., interleukin-2, bleomycin, ifosfamide, mesna, altretamine, topotecan, cytarabine, methylprednisolone, dexamethasone, mercaptopurine, thioguanine, fludarabine, gemtuzumab, idarubicin, mitoxantrone, tretinoin, alemtuzumab, chlorambucil, cladribine, imatinib, epirubicin, dacarbazine, procarbazine, mechlorethamine, rituximab, denileukin diftitox, allopurinol, carmustine, tamoxifen, filgrastim, temozolomide, melphalan, vinorelbine, azacitidine, thalidomide, and mitomycin.

14. The pharmaceutical composition according to claim 11, wherein said liposome further comprises sugars.

15. A peptide compound comprising a hydrophilic amino acid block and a hydrophobic amino acid block; wherein a) the peptide compound consists of 24 to 36 amino acids in total; b) the hydrophilic amino acid block consists of 4 to 10 amino acids in total and has an average hydropathy index of -3.0 to -1.0; and c) the hydrophobic amino acid block consists of 20 to 32 amino acids in total, containing one or more His residues, and having an average hydropathy index of 1.0 to 2.5, wherein the hydrophobic amino acid block contains 5 to 8 units represented by the following formula (II): (AA.sub.5)(AA.sub.6)(AA.sub.7)(AA.sub.8) (II) wherein AA.sub.5, AA.sub.6, AA.sub.7, and AA.sub.8 are the same or different, and each represents His, Leu, or Ala, wherein when the hydrophobic amino acid block contains two or more His residues, no His residues between the units or in each unit are adjacent to each other; and wherein each unit may have the same or different amino acid sequences.

16. A liposome comprising the peptide compound according to claim 15, and a lipid.

Summary for Patent: ► Subscribe

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan2012-233011Oct 22, 2012
PCT Information
PCT FiledOctober 21, 2013PCT Application Number:PCT/JP2013/078497
PCT Publication Date:May 01, 2014PCT Publication Number: WO2014/065245

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Inventors Patent Expiration Status Orphan Source
Amgen
NEUPOGEN
filgrastim
VIAL1033530011991-02-20► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXsearch
Amgen
NEUPOGEN
filgrastim
VIAL1033530021991-02-20► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXsearch
Amgen
NEUPOGEN
filgrastim
SYRINGE1033530031991-02-20► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXsearch
Amgen
NEUPOGEN
filgrastim
SYRINGE1033530041991-02-20► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXsearch
Genentech
RITUXAN
rituximab
VIAL1037050011997-11-26► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXsearch
Eisai Inc
ONTAK
denileukin diftitox
VIAL1037670011999-02-05► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXOrphansearch
Genentech
HERCEPTIN
trastuzumab
VIAL; INTRAVENOUS1037920011998-09-25► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXOrphansearch
Genzyme
CAMPATH
alemtuzumab
VIAL; INTRAVENOUS1039480012001-05-07► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXOrphansearch
Genzyme
CAMPATH
alemtuzumab
VIAL; INTRAVENOUS1039480022001-05-07► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXOrphansearch
Genzyme
LEMTRADA
alemtuzumab
INJECTABLE;INJECTION1039480032001-05-07► Subscribe Taiho Pharmaceutical Co., Ltd. (Tokyo, JP) Kogure; Kentaro (Otsu, JP), Hama; Susumu (Otsu, JP) ► SubscribeRXOrphansearch
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