Pimicotinib is the first highly selective CSF-1R inhibitor discovered by a Chinese company that entered into a global phase III clinical trial. The study is also the first global Phase III study of TGCT to be conducted simultaneously in China, US and Europe. Approximately 100 participants are p...
12 June 2023, Shanghai – Abbisko Therapeutics Co., Ltd. (“Abbisko Therapeutics”hereafter) today announced that the first patient has been dosed in the phase II trial evaluating its CSF-1R inhibitor, Pimicotinib (ABSK021), in patients with cGVHD. The primary underlying mechanism of cGVHD is...
Background: NMS-03592088 is a novel, potent inhibitor of the FLT3, CSF1R and KIT receptor tyrosine kinases (KD < 1 nM for all three targets). The compound demonstrated high preclinical efficacy following oral administration in all tested target-dependent tumor models, including those harboring ...
On January 9, 2024, Abbisko Therapeutics (HKEX code: 02256) announced that its investigational innovative CSF-1R inhibitor pimicotinib(ABSK021) has been granted orphan drug designation(ODD) by the European Medicines Agency (EMA) for the treatment of inoperable tenosynovial giant cell tumor (TGCT)...
(Abbisko Therapeutics) today announced that its CSF-1R inhibitor pimicotinib(ABSK021)has been granted the fast track designation(FTD) by the U.S. FDA for the treatment of tenosynovial giant cell tumor (TGCT) patients that are not amenable to surgery. Previously, pimicotinib was granted the ...
The small molecule PLX5622, a highly selective inhibitor of CSF1R kinase, has been used to deplete microglia and, thereby, alter energy intake and expenditure in high-fat-diet (HFD)-fed mice [9, 10]. Recent data suggest that the effect of PLX5622 is not restricted to microglia and that...
Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necr
For the (−)-kusunokinin target protein, the docking result of (−)-kusunokinin had to show lower ΔGbind and Ki towards the target protein, compared to the docking result of the known inhibitor with its counterpart. The 51 potential targets in which the ΔGbind of kusunokinin was ...
Using a structure-guided drug design strategy based on the existing CSF1R/KIT/FLT3 inhibitor PLX339710,18, combined with in vivo screening for optimal PK, brain penetrance, and microglial depletion, we created PLX5622 (Fig. 2a), with crystallography revealing the interactions between PLX5622 and...
(co-therapeutics) can be used simultaneously with the CSF-1R inhibitor as by concurrent administration, admixing the cotherapeutic with the CSF-1R inhibitor, or by sequential administration. A preferred embodiment involves use of a compound selected from those of Formula I disclosed herein, (e.g...