[Translation] A multi-center, multi-stage clinical study to evaluate the safety and efficacy of subretinal injection of LX102 in subjects with neovascular age-related macular degeneration

评价视网膜下注射LX102治疗新生血管性年龄相关性黄斑变性（nAMD）的总体安全性和有效性

[Translation]

To evaluate the overall safety and efficacy of subretinal injection of LX102 in the treatment of neovascular age-related macular degeneration (nAMD)

Start Date-

Sponsor / Collaborator

Innostellar Biotherapeutics Co., Ltd.Ltd.

NCT05831007 / Active, not recruitingNot ApplicableIIT

An Open Label Dose Escalation Clinical Trial to Evaluate the Safety and the Efficacy of LX102-C01 in Patients With Neovascular Age-Related Macular Degeneration (nAMD)

The goal of this study is to evaluate the safety and efficacy of LX102-C01 treatment of nAMD. This study will enroll subjects aged ≥ 50 years old to receive a single unilateral intravitreal (IVT) injection of LX102-C01 to evaluate its safety and efficacy.

Start Date06 Dec 2021

Sponsor / Collaborator

Shanghai First People's Hospital

[+1]

100 Clinical Results associated with LX102(Innostellar)

100 Translational Medicine associated with LX102(Innostellar)

100 Patents (Medical) associated with LX102(Innostellar)

Literatures (Medical) associated with LX102(Innostellar)

01 Oct 2019·ChemBioChemQ4 · BIOLOGY

Rational Design and Identification of Small‐Molecule Allosteric Inhibitors of CD38

Q4 · BIOLOGY

Article

Author: Jin, Hongwei ; Shi, Xiaomeng ; Zhang, Lihe ; Li, Ting ; Liu, Zhenming ; Zhao, Yongjuan ; Wu, Yang ; Yang, Lixin ; Lee, Hon Cheung ; Zhang, Liangren ; Li, Songlu

AbstractCD38 is a multi‐functional signaling enzyme that catalyzes the biosynthesis of two calcium‐mobilizing second messengers: cyclic ADP‐ribose and nicotinic acid adenine dinucleotide phosphate. It also regulates intracellular nicotinamide adenine dinucleotide (NAD) contents, associated with multiple pathophysiological processes such as aging and cancer. As such, enzymatic inhibitors of CD38 offer great potential in drug development. Here, through virtual screening and enzymatic assays, we discovered compound LX‐102, which targets CD38 on the side opposite its enzymatic pocket with a binding affinity of 7.7 μm. It inhibits the NADase activity of CD38 with an IC50 of 14.9 μm. Surface plasmon resonance (SPR) and hydrogen/deuterium exchange and mass spectrometry experiments verified that LX‐102 competitively binds to the epitope of the therapeutic SAR 650984 antibody in an allosteric manner. Molecular dynamics simulation was performed to demonstrate the binding dynamics of CD38 with the allosteric ligand. In summary, we established that the cavity to which SAR 650984 binds was an allosteric site and was accessible for the rational design of small chemical modulators of CD38. The lead compound LX‐102 that we identified in this study could also be a useful tool for probing CD38 functions and promoting drug discovery.

100 Deals associated with LX102(Innostellar)

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Wet age-related macular degeneration	Phase 2	CN	Innostellar Biotherapeutics Co., Ltd.Ltd.	19 Jan 2023

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