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

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5365—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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
    • A61K47/64—Drug-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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/083—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being octreotide or a somatostatin-receptor-binding peptide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules 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
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones

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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3801506A4 (en) * 2018-06-01 2022-08-10 Tva (Abc), Llc Combination therapy
CA3133798A1 (en) * 2019-03-18 2020-09-24 The Trustees Of Columbia University In The City Of New York Non-hydrolyzable, non-cleavable, stable linkers for precision therapeutics and uses thereof
US20220257766A1 (en) * 2019-06-25 2022-08-18 Tva (Abc), Llc 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

Family Cites Families (10)

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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
MX2010012124A (en) * 2008-05-14 2011-04-05 Ipsen Pharma Sas 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
US10925978B2 (en) 2014-01-29 2021-02-23 Cosmo Technologies Limited 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
WO2016004043A1 (en) * 2014-06-30 2016-01-07 Blend Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
EP3160518A4 (en) * 2014-06-30 2018-05-23 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
WO2017003940A1 (en) 2015-06-30 2017-01-05 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof

Also Published As

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

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