ATLAS-101 is a Phase I/II clinical trial of AMXI-5001 in adult participants with advanced malignancies who have previously failed other therapies. The study has two phases. The purpose of Phase I (Dose Escalation) is to confirm the appropriate treatment dose and Phase II (Dose Expansion) is to characterize the safety and efficacy of AMXI-5001.

Start Date12 Aug 2020

Sponsor / Collaborator

Atlasmedx, Inc.

100 Clinical Results associated with PARP1 x PARP2 x Tubulin

100 Translational Medicine associated with PARP1 x PARP2 x Tubulin

0 Patents (Medical) associated with PARP1 x PARP2 x Tubulin

Literatures (Medical) associated with PARP1 x PARP2 x Tubulin

31 Dec 2023·Journal of Enzyme Inhibition and Medicinal Chemistry

Flavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer

Article

Author: Naik, Aliva ; Sharma, Ram ; Sharma, Anamika ; Sharma, Sachin ; Banerjee, Arnab ; Liou, Jing Ping ; Guru, Santosh Kumar ; Nepali, Kunal ; Grewal, Ajmer Singh ; Dhingra, Ashwani K. ; Chandra, Kavya ; Thakur, Amandeep

Structural tailoring of the flavone framework (position 7) via organopalladium-catalyzed C-C bond formation was attempted in this study. The impact of substituents with varied electronic effects (phenyl ring, position 2 of the benzopyran scaffold) on the antitumor properties was also assessed. Resultantly, the efforts yielded a furyl arm bearing benzopyran possessing a 4-fluoro phenyl ring (position 2) (14) that manifested a magnificent antitumor profile against the Ishikawa cell lines mediated through dual inhibition of PARP and tubulin [(IC₅₀ (PARP1) = 74 nM, IC₅₀ (PARP2) = 109 nM) and tubulin (IC₅₀ = 1.4 µM)]. Further investigations confirmed the ability of 14 to induce apoptosis as well as autophagy and cause cell cycle arrest at the G2/M phase. Overall, the outcome of the study culminated in a tractable dual PARP-tubulin inhibitor endowed with an impressive activity profile against endometrial cancer.

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