CPL304110 News - LARVOL Sigma

|||||||||| Recentin (cediranib) / AstraZeneca, fexagratinib (ABSK091) / Abbisko, CPL304110 / Celon Labs
Preclinical, Journal: Fibroblast Growth Factor Receptor Inhibitors Decrease Proliferation of Melanoma Cell Lines and Their Activity Is Modulated by Vitamin D. (Pubmed Central) - Mar 17, 2024
In this study, we explored the response of A375 and RPMI7951 melanoma lines to CPL304110 (CPL110), a novel selective inhibitor of fibroblast growth factor receptors (FGFRs), and compared its efficacy with that of AZD4547, the first-generation FGFRs selective inhibitor...Interestingly, 1,25(OH)2D3 and CPL304110 co-treatment resulted in activation of the ERK1/2 pathway in A375 cells. Our results strongly suggested possible crosstalk between vitamin D-activated pathways and activity of FGFR inhibitors, which should be considered in further clinical studies.

||||||||||  CPL304110 / Celon Pharma
Trial completion date, Trial primary completion date, Metastases:  Safety, Tolerability and Pharmacokinetics of Oral CPL304110, in Adult Subjects With Advanced Solid Malignancies (clinicaltrials.gov) -  Feb 15, 2024
P1, N=42, Recruiting,  Sponsor: Celon Pharma SA
Our results strongly suggested possible crosstalk between vitamin D-activated pathways and activity of FGFR inhibitors, which should be considered in further clinical studies. Trial completion date: Dec 2023 --> Jun 2024 | Trial primary completion date: Dec 2023 --> Jun 2024

|||||||||| Balversa (erdafitinib) / J&J, Pemazyre (pemigatinib) / Incyte, Specialised Therap
Preclinical, Journal: Preclinical characterization of CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3 for gastric, bladder, and squamous cell lung cancer. (Pubmed Central) - Jan 29, 2024
P1
Comparative analyses with FDA-approved FGFR inhibitors, erdafitinib and pemigatinib, revealed certain advantages of CPL304110 in both in vitro and in vivo assessments. Encouraging preclinical results led the way for the initiation of a Phase I clinical trial (01FGFR2018; NCT04149691) to further evaluate CPL304110 as a novel anticancer therapy.

||||||||||  CPL304110 / Celon Pharma
Trial completion date, Trial primary completion date, Metastases:  Safety, Tolerability and Pharmacokinetics of Oral CPL304110, in Adult Subjects With Advanced Solid Malignancies (clinicaltrials.gov) -  Feb 27, 2023
P1, N=42, Recruiting,  Sponsor: Celon Pharma SA
Encouraging preclinical results led the way for the initiation of a Phase I clinical trial (01FGFR2018; NCT04149691) to further evaluate CPL304110 as a novel anticancer therapy. Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Dec 2022 --> Dec 2023

|||||||||| CPL304110 / Celon Labs
Preliminary results from a phase IA trial of selective FGFR1-3 inhibitor CPL304110 in patients with FGFR-deregulated advanced solid malignancies (Amphitheatre Bordeaux) - Jan 26, 2023 - Abstract #ESMOTAT2023ESMO_TAT_110;
P1
Conclusions The above early study observations suggest that CPL304110 administration is associated with acceptable toxicity and encouraging response rate in heavily pretreated patients with FGFR-aberrant advanced solid malignancies. The final selection of RP2D will take place after the end of phase IB.

||||||||||  CPL304110 / Celon Pharma
Trial completion date, Trial primary completion date, Metastases:  Safety, Tolerability and Pharmacokinetics of Oral CPL304110, in Adult Subjects With Advanced Solid Malignancies (clinicaltrials.gov) -  Mar 24, 2022
P1, N=42, Recruiting,  Sponsor: Celon Pharma SA
The final selection of RP2D will take place after the end of phase IB. Trial completion date: Jul 2021 --> Dec 2022 | Trial primary completion date: Jul 2021 --> Dec 2022

|||||||||| CPL304110 / Celon Labs
Biomarker, Journal: p38 Mediates Resistance to FGFR Inhibition in Non-Small Cell Lung Cancer. (Pubmed Central) - Jan 20, 2022
Here, we investigated the NSCLC cell lines response and potential mechanism of acquired resistance to novel selective FGFR inhibitor CPL304110...Moreover, the overexpression of this kinase in parental cells led to impaired response to FGFR inhibition, thus confirming that p38 MAPK is a driver of resistance to a novel FGFR inhibitor. Taken together, our results provide an insight into the potential direction for NSCLC targeted therapy.

|||||||||| CPL304110 / Celon Labs
Preclinical, Journal: MET-Pyk2 Axis Mediates Acquired Resistance to FGFR Inhibition in Cancer Cells. (Pubmed Central) - Apr 27, 2021
In this study, we focused on a novel pan-FGFR inhibitor-CPL304110, currently being investigated in phase I clinical trials in adults with advanced solid malignancies...Our results demonstrate that the HGF/MET-Pyk2 signaling axis confers resistance to the novel FGFR inhibitor, and this mechanism is common for lung, gastric, and bladder cancer cells. Our study suggests that targeting of MET/Pyk2 could be an approach to overcome resistance to FGFR inhibition.

|||||||||| CPL304110 / Celon Labs
Review, Journal: Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). (Pubmed Central) - Apr 23, 2021
P1
Compound 56q (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, -2, -3 with ICs of 0.75 nM, 0.50 nM, 3.05 nM respectively, whereas IC of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in vivo, compound 56q is currently under evaluation in phase I clinical trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691).

||||||||||  CPL304110 / Celon Pharma
Trial completion date, Trial primary completion date, Metastases:  Safety, Tolerability and Pharmacokinetics of Oral CPL304110, in Adult Subjects With Advanced Solid Malignancies (clinicaltrials.gov) -  Oct 29, 2020
P1, N=42, Recruiting,  Sponsor: Celon Pharma SA
Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in vivo, compound 56q is currently under evaluation in phase I clinical trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691). Trial completion date: Jul 2020 --> Jul 2021 | Trial primary completion date: Jul 2020 --> Jul 2021

|||||||||| CPL304110 / Celon Labs
[VIRTUAL] Preclinical characterization of CPL304110 as a potential selective inhibitor of fibroblast growth factors 1/2/3 in solid cancers (On-Demand) - Jul 21, 2020 - Abstract #ESMO2020ESMO_831;
P1
Our drug is currently under clinical investigation – Phase I (NCT04149691). Legal entity responsible for the study: Celon Pharma S.A. Funding: Celon Pharma S.A and NCBR grant.

||||||||||  CPL304110 / Celon Pharma
New P1 trial, Metastases:  Safety, Tolerability and Pharmacokinetics of Oral CPL304110, in Adult Subjects With Advanced Solid Malignancies (clinicaltrials.gov) -  Nov 14, 2019
P1, N=42, Recruiting,  Sponsor: Celon Pharma SA



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