Delving into the Latest Updates on ODM-203 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Mechanism

FGFRs antagonists(Fibroblast growth factor receptors antagonists), VEGFR antagonists(Vascular endothelial growth factor receptor antagonists)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [1]

Active Indication

Colorectal CancerKidney NeoplasmsOvarian Cancer+ [1]

Inactive Indication

Advanced Malignant Solid Neoplasm

Originator Organization

Orion Oyj

Active Organization

Aurigene Oncology Ltd.

Orion Oyj

Inactive Organization

Orion Corp.

Orion Pharma Ltd.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC26H21F2N5O2S

InChIKeyZJFCBQXPTQSTCZ-UHFFFAOYSA-N

CAS Registry1430723-35-5

This is an open-label, multicentre, randomized, Phase II study and will be conducted with co-primary objectives of the study are to assess the efficacy of AUR109, as measured by ORR and safety / tolerability at three different dose levels of the study drug in three cancer indications i.e., colorectal, ovarian cancer and renal cancer.

Start Date09 Nov 2024

Sponsor / Collaborator

Aurigene Oncology Ltd.

CTRI/2021/11/038092

/ RecruitingPhase 2

A Phase II Open-Label Trial Evaluating the Efficacy and Safety of Once Daily Oral ODM-203 in Patients with Unresectable Transitional Cell Urothelial Carcinoma with FGFR3 Mutation - TEJAS-1

Start Date23 Dec 2021

Sponsor / Collaborator-

NCT03240445

/ CompletedPhase 1

A Part-randomised, Single Centre, Single Dose, Crossover,Phase I Study to Investigate the Impact of Changes to the Dosing Regimen on the Pharmacokinetic Profile of ODM-203 in Healthy Male Volunteers

This Phase I study in healthy male volunteers will evaluate the impact of the effect of food on the pharmacokinetic profile of ODM-203.

Start Date24 Aug 2017

Sponsor / Collaborator

Orion Corp.

[+1]

100 Clinical Results associated with ODM-203

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100 Translational Medicine associated with ODM-203

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100 Patents (Medical) associated with ODM-203

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4

Literatures (Medical) associated with ODM-203

01 Sep 2021·International Journal of PharmaceuticsQ2 · MEDICINE

How to stop disproportionation of a hydrochloride salt of a very weakly basic compound in a non-clinical suspension formulation

Q2 · MEDICINE

Article

Author: Malmström, Chira ; Bansal, Indu ; Shevchenko, Anna ; Korjamo, Timo ; Laakso, Sirpa ; Salmia, Jukka ; van Veen, Bert ; Samiulla, D S ; Juppo, Anne ; Koistinen, Piritta ; Ylikotila, Johanna ; Ojala, Krista

Our objectives were to stabilize a non-clinical suspension for use in toxicological studies and to develop methods to investigate the stability of the formulation in terms of salt disproportionation. The compound under research was a hydrochloride salt of a practically insoluble discovery compound ODM-203. The first of the three formulation approaches was a suspension prepared and stored at room temperature. The second formulation was stabilized by pH adjustment. In the third approach cooling was used to prevent salt disproportionation. 5 mg/mL aqueous suspension consisting of 20 mg/mL PVP/VA and 5 mg/mL Tween 80 was prepared for each of the approaches. The polymer was used as precipitation inhibitor to provide prolonged supersaturation while Tween 80 was used to enhance dissolution and homogeneity of the suspension. The consequences of salt disproportionation were studied by a small-scale in vitro dissolution method and by an in vivo pharmacokinetic study in rats. Our results show that disproportionation was successfully suppressed by applying cooling of the suspension in an ice bath at 2-8 °C. This procedure enabled us to proceed to the toxicological studies in rats. The in vivo study results obtained for the practically insoluble compound showed adequate exposures with acceptable variation at each dose level.

01 Jan 2020·ESMO OpenQ3 · MEDICINE

Phase I/IIa, open-label, multicentre study to evaluate the optimal dosing and safety of ODM-203 in patients with advanced or metastatic solid tumours

Q3 · MEDICINE

ArticleOA

Author: Giuseppe Curigliano ; Christophe Massard ; Analía Azaro ; Ulrik Lassen ; Antoine Italiano ; Pasi Hakulinen ; Mika V.J. Mustonen ; Katriina J. Peltola ; Rebecca S. Kristeleit ; Petri Bono ; Tarja Ikonen ; Jordi A. Rodon ; Hendrik Tobias Arkenau ; Chris Garratt

BACKGROUNDGenetic alterations in fibroblast growth factor receptor (FGFR) and vascular endothelial growth factor receptor (VEGFR) signalling are observed in various tumours. We report a first-in-human phase I/IIa trial evaluating tolerability, pharmacokinetics and preliminary antitumour activity of ODM-203, a novel FGFR and VEGFR inhibitor.METHODSOpen-label, non-randomised, multicentre, phase I/IIa dose escalation and expansion study in patients with advanced or metastatic solid tumours.RESULTSOverall, 84 patients received treatment; optimal tablet dose was found to be 400 mg/day with food. All patients experienced at least one adverse event; the majority (89.2%) were grade 1 or 2% and 70.4% were considered treatment related. The most commonly reported events were bilirubin increase-related events (75%) and diarrhoea (50%).Overall response rate was 9.2% and median progression-free survival was 16.1 and 12.4 weeks for patients with aberrant or non-aberrant FGFR tumours. Median time on treatment was 10.1 weeks for all patients and 14.5 weeks for patients who received 400 mg tablets.CONCLUSIONThis study suggests ODM-203 400 mg/day results in sufficient plasma concentrations and acceptable tolerability in most patients. Preliminary signs of therapeutic activity of ODM-203 in patients with solid tumours was observed.TRIAL REGISTRATION NUMBERNCT02264418.

01 Jan 2019·Molecular Cancer TherapeuticsQ2 · MEDICINE

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

Q2 · MEDICINE

Article

Author: Wohlfahrt, Gerd ; Linnanen, Tero ; Ikonen, Tarja ; Ramachandra, Murali ; Narayanan, Kishore ; Anthony, Thomas ; Oksala, Riikka ; Björkman, Mari L. ; Moilanen, Anu-Maarit ; Srinivas, Nanduri ; Ramachandra, Raghuveer K. ; Mukherjee, Subhendu ; Karlsson, Stefan ; Korjamo, Timo ; Rajagopalan, Srinivasan ; Holmström, Tim H. ; Kallio, Pekka J. ; Dhodheri, Samiulla ; Nair, Rashmi ; Samajdar, Susanta ; Ujjinamatada, Ravi K. ; Chelur, Shekar ; Mani, Jiju ; Gowda, Nagaraj

AbstractAlterations in the gene encoding for the FGFR and upregulation of the VEGFR are found often in cancer, which correlate with disease progression and unfavorable survival. In addition, FGFR and VEGFR signaling synergistically promote tumor angiogenesis, and activation of FGFR signaling has been described as functional compensatory angiogenic signal following development of resistance to VEGFR inhibition. Several selective small-molecule FGFR kinase inhibitors are currently in clinical development. ODM-203 is a novel, selective, and equipotent inhibitor of the FGFR and VEGFR families. In this report we show that ODM-203 inhibits FGFR and VEGFR family kinases selectively and with equal potency in the low nanomolar range (IC50 6–35 nmol/L) in biochemical assays. In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines (IC50 50–150 nmol/L). In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. In addition, ODM-203 inhibits metastatic tumor growth in a highly angiogenesis-dependent kidney capsule syngenic model. Interestingly, potent antitumor activity in the subcutaneous syngenic model correlated well with immune modulation in the tumor microenvironment as indicated by marked decrease in the expression of immune check points PD-1 and PD-L1 on CD8 T cells and NK cells, and increased activation of CD8 T cells. In summary, ODM-203 shows equipotent activity for both FGFR and VEGFR kinase families and antitumor activity in both FGFR and angigogenesis models.

100 Deals associated with ODM-203

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 2	IN	Aurigene Oncology Ltd.	09 Nov 2024
Kidney Neoplasms	Phase 2	IN	Aurigene Oncology Ltd.	09 Nov 2024
Ovarian Cancer	Phase 2	IN	Aurigene Oncology Ltd.	09 Nov 2024
Neoplasms	Phase 2	-	Orion Oyj	-
Solid tumor	Discovery	FI	Orion Oyj	21 Apr 2016
Advanced Malignant Solid Neoplasm	Discovery	DK	Orion Corp.	18 Sep 2014
Advanced Malignant Solid Neoplasm	Discovery	IT	Orion Corp.	18 Sep 2014
Advanced Malignant Solid Neoplasm	Discovery	FR	Orion Corp.	18 Sep 2014
Advanced Malignant Solid Neoplasm	Discovery	ES	Orion Corp.	18 Sep 2014
Advanced Malignant Solid Neoplasm	Discovery	GB	Orion Corp.	18 Sep 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02264418 (Pubmed \| ESMO Open) Manual	Phase 1/2	Neoplasms	84	ODM-203	(wqrdfsubkk) = hhmwlpbblg ibbnxhkund (vjgcsqltyy ) View more	Positive	01 Dec 2020
NCT02264418 (KIDES, ESMO2018)	Phase 1/2	Advanced Malignant Solid Neoplasm	84	ODM-203	(gzqcieybew) = 41% hkznbhfuvm (rakzdruqge ) View more	Positive	22 Oct 2018