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SG11201903431SA - Sstr-targeted conjugates and particles and formulations thereof - Google Patents

Sstr-targeted conjugates and particles and formulations thereof

Info

Publication number
SG11201903431SA
SG11201903431SA SG11201903431SA SG11201903431SA SG11201903431SA SG 11201903431S A SG11201903431S A SG 11201903431SA SG 11201903431S A SG11201903431S A SG 11201903431SA SG 11201903431S A SG11201903431S A SG 11201903431SA SG 11201903431S A SG11201903431S A SG 11201903431SA
Authority
SG
Singapore
Prior art keywords
international
conjugates
conj
massachusetts
particles
Prior art date
Application number
SG11201903431SA
Inventor
Rajesh R Shinde
Rossitza G Alargova
Soo Patrick Lim
Beata Sweryda-Krawiec
Leila Alland
Chris Sears
Original Assignee
Tarveda Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Tarveda Therapeutics Inc filed Critical Tarveda Therapeutics Inc
Publication of SG11201903431SA publication Critical patent/SG11201903431SA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/083Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being octreotide or a somatostatin-receptor-binding peptide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5015Organic compounds, e.g. fats, sugars
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72Receptors; Cell surface antigens; Cell surface determinants for hormones

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Zoology (AREA)
  • Endocrinology (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • General Preparation And Processing Of Foods (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MUNRO III HO I1111 011001 0 01111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2018/081521 Al 03 May 2018 (03.05.2018) WIP0 I PCT (51) International Patent Classification: House Rd, Bernardsville, New Jersey 07924 (US). SEARS, A61K 47/64 (2017.01) C07K 14/72 (2006.01) Chris; 3 Leslie Rd., Belmont, Massachusetts 02478 (US). A61P 35/00 (2006.01) (74) Agent: WARD, Donna T. et al.; DT WARD, PC, 142A (21) International Application Number: Main Street, Groton, Massachusetts 01450 (US). PCT/US2017/058701 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 27 October 2017 (27.10.2017) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (25) Filing Language: English DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (26) Publication Language: English HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, (30) Priority Data: KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 62/414,481 28 October 2016 (28.10.2016) US MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (71) Applicant: TARVEDA THERAPEUTICS, INC. SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, [US/US]; 134 Coolidge Avenue, Watertown, Massachusetts TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. 02472 (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: SHINDE, Rajesh R.; 110 Stearns Hill Rd, kind of regional protection available): ARIPO (BW, GH, Waltham, Massachusetts 02451 (US). ALARGOVA, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, _ Rossitza G.; 148 Newton St., Apt.4, Brighton, Massachu- UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, setts 02135 (US). LIM SOO, Patrick; 64 Garfield Place, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = Unit B, Ridgewood, New Jersey 07450 (US). SWERY- EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, DA-KRAWIEC, Beata; 46 Littlefield Lane, Marlborough, = Massachusetts 01752 (US). ALLAND, Leila; 102 Carriage = (54) Title: SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF Fig. 3 HCC-33 Xenograft efficacy Vehicle 4 wikm. = 2000 *).0.:. Conj. 57 1.0mg/kg = — 1800 .. % 1600 i Conj. 57 0.5mg/kg = — E 1400 . Conj. 57 0.33mg/kg ..,,,.. ' I ' = 1200 i , ...e. , Conj. 57 O.Smg/kg2x's/week = '5 1000 > Conj. 57 0.25mg/kg2x's/week E 800 = 2 - 600 = (i.i °.° 400 • w 200 > .' _ — 0 ,. , 1-1 0 3 6 9 12 15 18 21 24 27 30 Days 1-1 ei kr) 1-1 (57) : Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding C moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved - --- GC temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of , 1 making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject 0 in need thereof are provided, for example, to treat or prevent cancer. ei O [Continued on next page] WO 2018/081521 Al MIDEDIMOM0101011EFIDINIRMEOHOIHOIIIMEMOIS TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3))
SG11201903431SA 2016-10-28 2017-10-27 Sstr-targeted conjugates and particles and formulations thereof SG11201903431SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662414481P 2016-10-28 2016-10-28
PCT/US2017/058701 WO2018081521A1 (en) 2016-10-28 2017-10-27 Sstr-targeted conjugates and particles and formulations thereof

Publications (1)

Publication Number Publication Date
SG11201903431SA true SG11201903431SA (en) 2019-05-30

Family

ID=62024057

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201903431SA SG11201903431SA (en) 2016-10-28 2017-10-27 Sstr-targeted conjugates and particles and formulations thereof

Country Status (12)

Country Link
US (2) US11213590B2 (en)
EP (1) EP3532104A4 (en)
JP (2) JP2019532091A (en)
KR (1) KR20190075938A (en)
CN (1) CN109890423A (en)
AU (1) AU2017348313B2 (en)
CA (1) CA3039065A1 (en)
IL (2) IL299532A (en)
MX (1) MX2019004963A (en)
SG (1) SG11201903431SA (en)
TW (1) TW201828992A (en)
WO (1) WO2018081521A1 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021525766A (en) * 2018-06-01 2021-09-27 ターベダ セラピューティクス インコーポレイテッドTarveda Therapeutics,Inc. Combination therapy
US20220008566A1 (en) * 2018-10-12 2022-01-13 Advanced Accelerator Applications International Sa Pharmaceutical Composition Comprising a Radiolabeled GRPR Antagonist and a Surfactant
JP2022525785A (en) * 2019-03-18 2022-05-19 ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク Non-hydrolyzable, non-cleavable, stable linker and its uses for precision treatment
CA3143373A1 (en) * 2019-06-25 2020-12-30 Tarveda Therapeutics, Inc. Sstr-targeted conjugates and formulations thereof
WO2022174171A1 (en) * 2021-02-15 2022-08-18 Anp Technologies, Inc. Pharmaceutical composition containing taxane nanoaggregates and use thereof
WO2022232124A1 (en) * 2021-04-26 2022-11-03 H. Lee Moffitt Cancer Center And Research Institute, Inc. Targeted alpha particle therapy for somatostatin receptor 2 positive neuroendocrine tumors and metastases
CN114748481B (en) * 2022-05-12 2023-12-05 中国人民解放军海军军医大学 Application of terluostat hippurate in preparing medicines for resisting tick-borne encephalitis virus, west nile virus, yellow fever virus and chikungunya fever virus infection
WO2024129614A1 (en) 2022-12-13 2024-06-20 Crinetics Pharmaceuticals, Inc. Somatostatin subtype-2 receptor (sst2r) targeted therapeutics and uses thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5998154A (en) * 1995-07-07 1999-12-07 The University Of Texas System Somatostatin receptor peptide antigens and antibodies
US7666424B2 (en) * 2001-10-17 2010-02-23 Sloan-Kettering Institute For Cancer Research Methods of preparing and using single chain anti-tumor antibodies
US20070025910A1 (en) * 2005-07-29 2007-02-01 Norenberg Jeffrey P Anticancer therapy
US20110065632A1 (en) * 2008-05-14 2011-03-17 Zheng Xin Dong Pharmaceutical compositions of somatostatin-dopamine conjugates
WO2012138537A1 (en) * 2011-04-01 2012-10-11 Immunogen, Inc. Compositions and methods for treatment of ovarian, peritoneal, and fallopian tube cancer
WO2013039916A1 (en) * 2011-09-12 2013-03-21 The United States Of America, Represented By The Secretary, Dept. Of Health And Human Services Compositions for and methods of treatment and enhanced detection of non-pituitary tumors
KR102344079B1 (en) * 2014-01-29 2021-12-29 코스모 테크놀러지스 리미티드 Liquid composition in the form of emulsion or microemulsion for rectal administration containing at least one dye, and its use in a diagnostic endoscopic procedure of sigmoid colon and/or rectum
BR212016030926U2 (en) * 2014-06-30 2018-05-29 Tarveda Therapeutics Inc target conjugates and particles and formulations thereof
EP3164420A4 (en) * 2014-06-30 2018-05-23 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
CA2988591A1 (en) * 2015-06-30 2017-01-05 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof

Also Published As

Publication number Publication date
US11213590B2 (en) 2022-01-04
IL265770A (en) 2019-06-30
CN109890423A (en) 2019-06-14
US20220054647A1 (en) 2022-02-24
EP3532104A4 (en) 2020-06-24
IL299532A (en) 2023-02-01
JP2023010992A (en) 2023-01-20
AU2017348313B2 (en) 2021-10-21
US20190262460A1 (en) 2019-08-29
KR20190075938A (en) 2019-07-01
CA3039065A1 (en) 2018-05-03
TW201828992A (en) 2018-08-16
JP2019532091A (en) 2019-11-07
WO2018081521A1 (en) 2018-05-03
MX2019004963A (en) 2019-09-26
AU2017348313A1 (en) 2019-04-18
EP3532104A1 (en) 2019-09-04

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