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HRP20231699T1 - Formulacije inhibitora amorfne kinaze i postupci njihove primjene - Google Patents

Formulacije inhibitora amorfne kinaze i postupci njihove primjene Download PDF

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Publication number
HRP20231699T1
HRP20231699T1 HRP20231699TT HRP20231699T HRP20231699T1 HR P20231699 T1 HRP20231699 T1 HR P20231699T1 HR P20231699T T HRP20231699T T HR P20231699TT HR P20231699 T HRP20231699 T HR P20231699T HR P20231699 T1 HRP20231699 T1 HR P20231699T1
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compound
cellulose acetate
succinate
dextran
poly
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HRP20231699TT
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Michael D. Kaufman
Scott Bone
Corey Bloom
Fred Jordan
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Deciphera Pharmaceuticals, Llc
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Priority claimed from PCT/US2020/067557 external-priority patent/WO2021138483A1/en
Publication of HRP20231699T1 publication Critical patent/HRP20231699T1/hr

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Claims (14)

1. Farmaceutski prihvatljiva kompozicija za oralno administriranje, pri čemu kompozicija sadrži: (i) čvrstu disperziju, pri čemu čvrsta disperzija sadrži: amorfni oblik spoja predstavljenog formulom (I): [image] i farmaceutski prihvatljiv polimer; i (ii) jedan ili više farmaceutski prihvatljivih ekscipijenasa.
2. Farmaceutski prihvatljiva kompozicija prema zahtjevu 1, pri čemu: (i) čvrsta disperzija nema više od oko 5% m/m bilo kojeg kristalnog oblika spoja; i/ili (ii) čvrsta disperzija u suštini nema količinu koja se može detektirati bilo kojeg kristalnog oblika spoja; i/ili (iii) amorfni oblik ima uzorak difrakcije X-zraka praha u suštini kao što je prikazan na slici 1; i/ili (iv) kompozicija ne sadrži više od oko 5% (m/m) bilo kojeg kristalnog oblika spoja u agregatu kada je izložena 60% ili 75% relativne vlažnosti na 25 °C tokom 1 mjeseca, 3 mjeseca ili 6 mjeseci; i/ili (v) kompozicija sadrži oko 10% do oko 30%, oko 20% do oko 30% ili oko 25% masenih spoja na osnovu ukupne mase čvrste disperzije.
3. Farmaceutski prihvatljiva kompozicija prema zahtjevu 1 ili zahtjevu 2, pri čemu je farmaceutski prihvatljiv polimer odabran iz grupe koja se sastoji od: polivinil pirolidona, polietilenoksida, polietilen glikola, poli(vinil pirolidon-ko-vinil acetata), polioksietilen-polioksipropilen blok kopolimera, graft kopolimera sačinjenih od polietilen glikola, polivinil kaprolaktama i polivinil acetata, polimetakrilata, polioksietilen alkil etara, polioksietilen ricinusovih ulja, polikaprolaktama, polimliječne kiseline, poliglikolne kiseline, poli(mliječna-glikolna) kiseline, lipida, celuloze, pululana, dekstrana, maltodekstrina, hijaluronske kiseline, polizijalne kiseline, hondroitin sulfata, heparina, fukoidana, pentozan polisulfata, spirulana, hidroksipropil metil celuloza acetat sukcinata, hidroksipropil metil celuloza propionat sukcinata, hidroksipropil metil celuloza ftalata, celuloza acetat ftalata, celuloza acetat trimelitata, metil celuloza acetat ftalata, hidroksipropil celuloza acetat ftalata, celuloza acetat tereftalata, celuloza acetat izoftalata, karboksimetil etilceluloze, hidroksipropil metilceluloze, hidroksipropil metilceluloza acetat ftalata, hidroksipropil metilceluloza propionat ftalata, hidroksipropil metilceluloza acetat trimelitata, hidroksipropil metilceluloza propionat trimelitata, celuloza acetat sukcinata, metil celuloza acetat sukcinata, dekstrana, dekstran acetata, dekstran propionata, dekstran sukcinata, dekstran acetat propionata, dekstran acetat sukcinata, dekstran propionat sukcinata, dekstran acetat propionat sukcinata, poli(metakrilna kiselina-ko-metil metakrilata) 1:1, poli(metakrilna kiselina-ko-metil metakrilata) 1:2, poli(metakrilna kiselina-ko-etil akrilata) 1: 1, hidroksietil celuloze, metil celuloze i hidroksi propil celuloze, poli metakrilna kiselina-etil akrilata, poli metakrilna kiselina-metil metakrilata, poli metil metakrilat-etil akrilata, poli trimetilamonioetil metakrilat hlorid-metil metakrilat-etil akrilata i poli(butilmetakrilat-ko-(2-dimetilaminoetil)metakrilat-ko-metil metakrilata), i njihovih smeša, na primjer u kojoj je farmaceutski prihvatljiv polimer odabran iz grupe koja se sastoji od: polivinil pirolidona, polietilenoksida, polietilen glikola, poli(vinil pirolidon-ko-vinil acetata), polioksietilen-polioksipropilen blok kopolimera, graft kopolimera sačinjenih od polietilen glikola, polivinil kaprolaktama i polivinil acetata, polimetakrilata, polioksietilen alkil etara, polioksietilen ricinusovih ulja, polikaprolaktama, polimliječne kiseline, poliglikolne kiseline, poli(mliječna-glikolna) kiseline, lipida, celuloze, pululana, dekstrana, maltodekstrina, hijaluronske kiseline, polizijalne kiseline, hondroitin sulfata, heparina, fukoidana, pentozan polisulfata, spirulana, hidroksipropil metil celuloza acetat sukcinata, hidroksipropil metil celuloza propionat sukcinata, hidroksipropil metil celuloza ftalata, celuloza acetat ftalata, celuloza acetat trimelitata, metil celuloza acetat ftalata, hidroksipropil celuloza acetat ftalata, celuloza acetat tereftalata, celuloza acetat izoftalata, karboksimetil etilceluloze, hidroksipropil metilceluloze, hidroksipropil metilceluloza acetat ftalata, hidroksipropil metilceluloza propionat ftalata, hidroksipropil metilceluloza acetat trimelitata, hidroksipropil metilceluloza propionat trimelitata, celuloza acetat sukcinata, metil celuloza acetat sukcinata, dekstrana, dekstran acetata, dekstran propionata, dekstran sukcinata dekstran acetat propionata, dekstran acetat sukcinata, dekstran propionat sukcinata, dekstran acetat propionat sukcinata, poli(metakrilna kiselina-ko-metil metakrilata) 1:1, poli(metakrilna kiselina-ko-metil metakrilata) 1:2, poli(metakrilna kiselina-ko-etil akrilata) 1: 1, i njihovih smjesa, kao što je u kojoj je farmaceutski prihvatljiv polimer hidroksipropil metil celuloza acetat sukcinat.
4. Farmaceutski prihvatljiva kompozicija prema bilo kojem od zahtjeva 1-3, pri čemu: (i) spoj i farmaceutski prihvatljiv polimer su prisutni u odnosu spoja:polimer od oko 40:60 do oko 10:90, od oko 30:70 do oko 20:80, ili oko 25:75; i/ili (ii) čvrsta disperzija je čvrsta disperzija osušena raspršivanjem; i/ili (iii) čvrsta disperzija ima topljivost u vodi na pH 6.5 od oko 120 µg/mL na 25 °C ili topljivost u vodi na pH 2 od oko 178 µg/mL na 25 °C; i/ili (iv) kompozicija sadrži manje od oko 10 %, manje od oko 3% ili manje od oko 1% masenih ili oko 0.1% masenih do oko 0.5% masenih ili oko 0.01% masenih do oko 0.1% masenih, spoja predstavljenog formulom (II): [image] na osnovu mase spoja formule (I).; i /ili (v) kompozicija sadrži manje od oko 10 %, manje od oko 3% ili manje od oko 1% masenih, ili oko 0.1% masenih do oko 0.5% masenih ili oko 0.01% masenih do oko 0.1% masenih spoja predstavljenog formulom (III): [image] na osnovu mase spoja formule (I).
5. Farmaceutski prihvatljiva kompozicija prema zahtjevu 1, koja je: (i) za oralnu isporuku pacijentu 50 mg spoja predstavljenog formulom (I), koje sadrži: intragranularnu mješavinu, pri čemu intragranularna mješavina sadrži: čvrstu disperziju koja ima 50 mg spoja pri čemu je spoj prisutan u amorfnom obliku, hidroksipropil metil celuloza acetat sukcinat; agens za povećanje zapremine i/ili punilac; i lubrikans i/ili sredstvo za klizanje; i ekstragranularnu mješavinu koja sadrži sredstvo za klizanje i/ili lubrikans; ili (ii) za oralnu isporuku pacijentu 50 mg spoja predstavljenog formulom (I), koje sadrži: čvrstu disperziju koja ima 50 mg spoja pri čemu je spoj prisutan u amorfnom obliku i hidroksipropil metil celuloza acetat sukcinat; agens za povećanje zapremine, punilac, i lubrikans i/ili sredstvo za klizanje; ili (iii) tableta koja ima 50 mg spoja predstavljenog formulom (I), koje sadrži: intragranularnu mješavinu, pri čemu intragranularna mješavina sadrži: čvrstu disperziju koja ima 50 mg spoja pri čemu je spoj prisutan u amorfnom obliku, i hidroksipropil metil celuloza acetat sukcinat; oko 25-35% masenih agensa za povećanje zapremine, na primjer mikrokristalnu celulozu, na osnovu ukupne količine farmaceutske kompozicije; oko 25-35% masenih punioca, na primjer laktoze ili njenog hidrata, na osnovu ukupne količine farmaceutske kompozicije; i ekstragranularnu mješavinu koja sadrži sredstvo za klizanje i/ili lubrikans.
6. Farmaceutski prihvatljiva kompozicija prema zahtjevu 1, koja je tableta koja ima 50 mg spoja predstavljenog formulom (I): [image] pri čemu tableta sadrži: čvrstu disperziju koja ima 50 mg spoja pri čemu je spoj prisutan u amorfnom obliku, i hidroksipropil metil celuloza acetat sukcinat; oko 25-35% masenih mikrokristalne celuloze na osnovu ukupne mase tablete; i oko 25-35% masenih laktoze ili njenog hidrata na osnovu ukupne količine farmaceutske kompozicije, po izboru gdje tableta dalje sadrži najmanje jedan od: magnezij stearata, krospovidona i silicij dioksida; i/ili se tableta raspadne za manje od 1 minuta testirano korištenjem USP <701> za neobložene tablete.
7. Farmaceutski prihvatljiva kompozicija prema zahtjevu 1, koja je za oralnu isporuku 50 mg spoja predstavljenog formulom (I), koje sadrži: intragranularnu mješavinu, pri čemu intragranularna mješavina sadrži: čvrstu disperziju koja ima 50 mg spoja pri čemu je spoj prisutan u amorfnom obliku i hidroksipropil metil celuloza acetat sukcinat; oko 25-35% masenih mikrokristalne celuloze na osnovu ukupne količine farmaceutske kompozicije; oko 25-35%% masenih laktoze ili njenog hidrata na osnovu ukupne količine farmaceutske kompozicije; oko 5% masenih krospovidona na osnovu ukupne količine farmaceutske kompozicije; oko 0.5% masenih silicijum dioksida na osnovu ukupne količine farmaceutske kompozicije; i oko 0.5% masenih magnezij stearata na osnovu ukupne količine farmaceutske kompozicije; i ekstragranularnu mješavinu koja sadrži oko 0.5% masenih silicij dioksida na osnovu ukupne količine farmaceutske kompozicije; i (ii) oko 0.5% masenih magnezij stearata na osnovu ukupne količine farmaceutske kompozicije.
8. Farmaceutski prihvatljiva kompozicija prema bilo kojem od zahtjeva 1-7, pri čemu kompozicija ili tableta oslobađa najmanje 80% spoja nakon 10 minuta do 40 minuta, na primjer nakon 20 minuta, kada je kompozicija testirana u 900 mL natrij acetatnog pufera na pH 4.5 korištenjem USP aparata II (metodom lopatica) na 37 °C, sa brzinom lopatica 75 ob/min.
9. Kompozicija kako je definirano u bilo kojem od zahtjeva 1 do 8 za primjenu u postupku liječenja bolesti odabrane iz grupe koja se sastoji od gastrointestinalnih stromalnih tumora (GIST), NF-1 deficijentnih gastrointestinalnih stromalnih tumora, sukcinat dehidrogenaza (SDH) deficijentnih gastrointestinalnih stromalnih tumora, gastrointestinalnih stromalnih tumora izazvanih KIT-om, gastrointestinalnih stromalnih tumora izazvanih PDGFRA-om, melanoma, akutne mijeloidne leukemije, tumora germinativnih stanica seminoma ili disgerminoma, mastocitoze, mastocitna leukemija, adenokarcinom pluća, rak skvamoznih stanica pluća, glioblastoma, glioma, pedijatrijskojeg glioma, astrocitoma, sarkoma, malignog sarkoma omotača perifernih nervnih ovojnica, sarkoma intime, hipereozinofilnog sindroma, idiopatskog hipereozinofilnog sindroma, kronične eozinofilne leukemije, akutne mijeloidne leukemije povezane sa eozinofilijom, limfoblastičnog T-staničnog limfoma, i raka pluća nemalih stanica kod pacijenta kome je to potrebno, koji obuhvaća administriranje pacijentu terapijski efikasne količine kompozicije
10. Kompozicija kako je definirano u bilo kojem od zahtjeva 1 do 8 za primjenu u postupku liječenja bolesti izabrane od: (i) grupe koja se sastoji od gastrointestinalnih stromalnih tumora (GIST), gastrointestinalnih stromalnih tumora izazvanih KIT-om, gastrointestinalnih stromalnih tumora izazvanih PDGFRA-om, raka pluća, glioblastoma, glioma, malignog sarkoma omotača perifernih nervnih ovojnica, i hipereozinofilnog sindroma; (ii) grupe koja se sastoji od tumora germinativnih stanica izazvanih KIT-om (npr., germinativnih stanica testisa), raka kože izazvanog KIT-om, ili karcinoma bubrežnih stanica izazvanog KIT-om; (iii) grupe koja se sastoji od raka penisa, raka penisa izazvanog PDGFRA-om, raka prostate, raka prostate izazvanog PDGFRA-om, nemelanomskog raka kože izazvanog PDGFRA-om, glioma izazvanog PDGFRA-om, sarkoma izazvanog PDGFRA-om, glioblastoma izazvanog PDGFRA-om, ili raka gušterače izazvanog PDGFRA-om; ili (iv) grupe koja se sastoji od raka vagine, raka prostate, raka penisa, nemelanomskog raka kože, melanoma, ili sarkoma dojke, pri čemu bolest sadrži PDGFRAB mutaciju, koji obuhvaća administriranje pacijentu terapijski efikasne količine kompozicije.
11. Kompozicija za primjenu prema zahtjevu 9, pri čemu je bolest gastrostromalni intestinalni tumori (GIST).
12. Kompozicija za primjenu prema bilo kojem od zahtjeva 9 - 11, pri čemu je bolest uzrokovana aktivnošću kinaze c-KIT i/ili PDGFRA, i/ili njihovim onkogenim oblicima.
13. Proces za pripremanje čvrste disperzije definirane u bilo kojem od zahtjeva 1 do 5, pri čemu proces obuhvaća: (a) mješanje spoja formule (I), otapala, polimera i vode da se dobije suspenzija; (b) po izboru agitiranje i/ili mješanje suspenzije uz održavanje temperature od oko 10 do oko 25 °C; (c) zagrijavanje suspenzije da se otope suspendirane čestice prije uvođenja u sušač raspršivanjem, po izboru gdje zagrijavanje obuhvaća prolaženje suspenzija kroz razmjenjivač topline u liniji; i (d) sušenje raspršivanjem suspenzije da se dobije disperzija sušena raspršivanjem; (e) sušenje disperzije sušene raspršivanjem; time dobivajući čvrstu disperziju.
14. Čvrsta disperzija koja sadrži amorfni oblik spoja formule (I) [image] proizvedena procesom prema zahtjevu 13.
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