Business Inquiry

Global：

Email:marketing@medicilon.com

+1(781)535-1428(U.S.)

0044 7790 816 954 (Europe)

China：

Email: marketing@medicilon.com.cn

Tel: +86 (21) 5859-1500

This site uses cookies and related technologies, as described in our privacy policy, for purposes that may include site operation, analytics, enhanced user experience, or advertising. You may choose to consent to our use of these technologies, or refuse these technologies

Syntheses, biological evaluations, and mechanistic studies of potent PD-L1 inhibitors with in vivo antitumor activity. PK studies were conducted by Medicilon

2023-07-11

Page View：

PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified compound L7 as a potent PD-L1 inhibitor that blocked PD-1/PD-L1 interaction. Pharmacokinetic (PK) studies demonstrated that L7 was orally bioavailable. PK studies were conducted by Medicilon.

Reference:

Liu Liu, et al. Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[ c][1,2,5]oxadiazole Derivatives as Potent PD-L1 Inhibitors with In Vivo Antitumor Activity. J Med Chem. 2021 Jun 24;64(12):8391-8409. doi: 10.1021/acs.jmedchem.1c00392.

PD-1-PD-L1 NSCLC PD-1/PD-L1-interaction Pharmacokinetic

Return

Relevant News

Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon

2023-07-11

The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.

SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties

2023-07-11

The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects. The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.

SKLB-YTH-60 ameliorates inflammation and fibrosis in Bleomycin-induced lung fibrosis mouse models. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon

2023-07-11

Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. YTH-60 has obvious anti‐proliferative activity on fibroblasts and A549 cells. YTH-60 has an acceptable oral bioavailability and appropriate eliminated half-life time. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon.