Pimicotinib Explained

Width:	200
Routes Of Administration:	Oral
Cas Number:	2253123-16-7
Pubchem:	139549388
Chemspiderid:	128942304
Unii:	HV1XI8HST2
Kegg:	D12938
Synonyms:	ABSK021
Iupac Name:	3,3-Dimethyl-N-[6-methyl-5-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxypyridin-2-yl]-2-oxopyrrolidine-1-carboxamide
C:	22
H:	24
N:	6
O:	3
Stdinchi:	1S/C22H24N6O3/c1-14-18(31-16-7-9-23-17(11-16)15-12-24-27(4)13-15)5-6-19(25-14)26-21(30)28-10-8-22(2,3)20(28)29/h5-7,9,11-13H,8,10H2,1-4H3,(H,25,26,30)
Stdinchikey:	NXFPMDWYDKHFMM-UHFFFAOYSA-N
Smiles:	CC1=C(C=CC(=N1)NC(=O)N2CCC(C2=O)(C)C)OC3=CC(=NC=C3)C4=CN(N=C4)C

Pimicotinib (ABSK021), an oral, highly potent and selective small molecule inhibitor of colony-stimulating factor 1 receptor (CSF-1R) independently discovered by Abbisko Therapeutics. A number of studies have shown that blocking the CSF-1R signaling pathway could effectively modulate and change macrophage functions, and potentially treat many macrophage-dependent human diseases.^[1]

History

In December 2023, Abbisko Therapeutics entered into a licensing agreement for pimicotinib in all indications for China rights with Merck KGaA.^{[2] [3] [4]}

In April 2023, a global phase III, randomized, double-blind, placebo-controlled, multicenter clinical trial designed to evaluate the safety and efficacy of pimicotinib in patients with tenosynovial giant cell tumor was started (NCT05804045).^[5]

Following with pimicotinib for tenosynovial giant cell tumor treatment in phase III, pimicotinib has also entered into a phase II trial in June 2023 for cGVHD treatment in China.^[6]

The U.S. Food and Drug Administration (FDA) and the Center for Drug Evaluation (CDE) of NMPA granted pimicotinib breakthrough therapy designation (BTD) for the treatment of tenosynovial giant cell tumor patients that are not amenable to surgery in January 2023 and July 2022, respectively.^[7]

Research

Pimicotinib is being investigated as a treatment for tenosynovial giant cell tumor,^{[8] [9]} chronic graft-versus-host-disease (cGVHD), and pancreatic cancer.

External links

• Web site: Pimicotinib . NCI Drug Dictionary . National Cancer Institute .

Notes and References

1. Vaynrub A, Healey JH, Tap W, Vaynrub M . Pexidartinib in the Management of Advanced Tenosynovial Giant Cell Tumor: Focus on Patient Selection and Special Considerations . OncoTargets and Therapy . 15 . 53–66 . 2022 . 35046667 . 8763255 . 10.2147/OTT.S345878 . free .
2. Merck Strengthens Oncology Portfolio Through Commercialization Agreement With Abbisko for Phase III Asset, Pimicotinib. (2023) https://www.merckgroup.com/en/news/abbisko-pimicotinib-agreement-04-12-2023.html
3. Merck KGaA buys into Abbisko's late-stage joint tumor med for $70M upfront. Fierce Biotech. (2023) https://www.fiercebiotech.com/biotech/merck-kgaa-buys-abbiskos-late-stage-joint-tumor-med-70m-upfront
4. Abbisko Therapeutics Announced the Entry into a Licensing Agreement for Pimicotinib (ABSK021) with Merck . www.prnewswire.com . 18 April 2024 .
5. Study of Pimicotinib (ABSK021) for Tenosynovial Giant Cell Tumor (MANEUVER). U. S. National Institutes of Health, National Cancer Institute. https://classic.clinicaltrials.gov/ct2/show/NCT05804045
6. A Phase II Study Evaluating the Efficacy and Safety of ABSK021 (Pimicotinib)) in the Treatment of cGvHD Chronic Graft Versus Host Disease (cGvHD)U. S. National Institutes of Health, National Cancer Institute.https://classic.clinicaltrials.gov/ct2/show/NCT06186804
7. Web site: FDA Grants Breakthrough Therapy Designation to Abbisko's Pimicotinib . Global genes . 18 April 2024.
8. Web site: Pimicotinib . TGCT Support . 18 April 2024 .
9. A Phase 3, Randomized, Double-blind, Placebo-Controlled, Multicenter Study of ABSK021 to Assess the Efficacy and Safety in Patients With Tenosynovial Giant Cell Tumor . clinicaltrials . clinicaltrials.gov . 18 April 2024 . 10 April 2024.