Merck Ua tiav Tiav Kev Txais Ntawm ArQule Thiab Tau Txais Lub Cim Tshiab Ntawm BTK Tus Ntxhw ARQ 531

Merck& Co tau tshaj tawm tias nws tau ua tiav qhov kev tau txais ntawm ArQule. Cov kev nrhiav tau tau tshaj tawm rau lub Kaum Ob Hlis 9, 2019. Merck, los ntawm lub chaw muag khoom, tau txais txhua qhov tshaj tawm ntawm ArQule rau Asmeskas $ 20 ntawm ib qhov rau kev yuav khoom tag nrho kwv yees li US $ 2. 7 nphom. Thaum lub sijhawm nrhiav tau, Merck' s lub chaw pabcuam tau sib xyaw rau hauv ArQule, uas tau dhau los ua tus tswv cuab ntawm Merck.

ArQule tsom rua kev tshawb pom thiab kev txhim kho ntawm kinase inhibitors rau kev kho mob qog noj ntshav thiab lwm yam kab mob. Lub tuam txhab' s tus neeg sib tw ua yeeb tshuaj tseem ceeb yog ARQ 531, qhov tshiab, qhov ncauj, thim rov qab Bruton tyrosine kinase (BTK) inhibitor muaj peev xwm tiv thaiv tsis tau hom tsiaj qus BTK thiab C 481 S mutant BTK. Lub C 481 S hloov pauv yog ib qho paub tiv cav ntawm thawj tiam ntawm kev tsis tuaj yeem hloov pauv BTK. Tam sim no, ARQ 531 yog nyob rau theem II koob tshuaj txuas ntxiv rau B-cell malignancies uas tau ua tsis tiav rau lwm yam kev kho mob.

Nyob rau ntawm 2019 American Society of Hematology (ASH) Lub Rooj Sib Tham Txhua Xyoo, ArQule tshaj tawm cov ntaub ntawv los ntawm Ntu I cov chaw sim tshuaj ntawm ARQ 531: 47 cov neeg mob uas rov mob / tso tawm qhov kabmob B-cell malignancies tau txais ntau koob ({{4),, 10, 1 5, 20, 30, 4 5, 6 5, 6 5, 7 {{4 }} mg, ib zaug ib hnub) ARQ 5 31 kev kho mob. Ntawm ntawm 9 cov neeg mob uas muaj mob rov huam dua qub / mob refractory mob qog ntshav qog ntshav (CLL) leej twg tau txais ib zaug ib hnub ntawm ≥6 5 mg thiab uas nws ua tau zoo tau raug soj ntsuam, 8 cov neeg mob tau txais cov lus teb ib nrab ( PR) nrog tus lej teb tag nrho (ORR) ntawm 89%. Tshwj xeeb, 8 ntawm 9 ntawm cov neeg mob uas muaj feem evaluable CLL nqa BTK-C 481 S hloov mus, thiab ntawm 7 ntawm lawv tau muaj qee yam kev zam txim.

Ntxiv nrog rau ARQ 531, muaj ntau lwm cov cuab tam hauv ArQule pipeline, suav nrog: (1) miransertib (ARQ {{{2}}), uas yog lub zog thiab xaiv AKT serine / threonine kinase inhibitor, tam sim no kev sim soj ntsuam I / Theem II (NCT {{3}}) yog tso npe rau cov neeg mob, suav nrog cov neeg mob Proteus syndrome thiab cov neeg mob PIK 3 CA-cuam tshuam txog tus kab mob overgrowth profile. (PROS); (2) ARQ75 1, lub cim tshiab ntawm cov muaj zog thiab xaiv AKT inhibitors, tam sim no Ib Theem I kev soj ntsuam kuaj mob (NCT0 2 76 1 694) yog tso npe rau cov neeg mob, tshwj xeeb cov neeg mob uas mob qog ntxig nqa PKD 3 CA / AKT / PTEN hloov pauv; (3) derazantinib, yias-FGFR (fibroblast growth factor receptor) inhibitor Tus Neeg Sawv Cev, tam sim no nyob rau Ntse I / II kho mob kho mob, rau kev kho mob ntawm FGFR-tsav intrahepatic cholangiocarcinoma (iCCA) thiab lwm yam mob qog nqaij hlav.

Dr. Roger M. Perlmutter, Thawj Tswj Hwm ntawm Merck Tshawb Fawb Chaw Soj Ntsuam, yav dhau los tau hais," ArQule' s tsom rua kev ntsuas tshuaj tau ua rau ntau theem kev kho mob ntawm qhov ncauj kinase inhibitors uas muaj cov khoom tshiab thiab cov khoom tseem ceeb. Qhov kev kis tau no yuav ua rau kom muaj cov cuab tam muaj txiaj ntsig Yuav ntxiv dag zog rau Merck' s kev sib txuas, feem ntau tshwj xeeb tshaj yog ARQ 531, cov neeg sib tw ua muaj tshuaj rau kev kho mob ntawm B-cell malignancies." (los ntawm Bioon.com, sau hsppharma.com)