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Highlight #2: Balversa (Erdafitinib)

Quinoxalines are common structural motifs found in a variety of biologically active compounds for anti-cancer, anti-inflammatory, antimalarial, anti-HIV and antimicrobial indications.[1] Janssen Oncology received approval from FDA for use of Balversa as a first targeted therapy for metastatic blood cancer in April, 2019.[2] Patients with locally advanced or metastatic urothelial carcinoma that has susceptible Fibroblast growth factor receptor 2 (FGFR2) or FGFR3 genetic alterations and that has progressed during or following prior platinum-containing chemotherapy were treated with this regimen. The efficacy studies of Balversa were conducted on selected 87 patients based on above criteria and results are promising with 2.3% patients having complete response and 30% showing partial response to the treatment.[3]

With more customised drugs becoming the standard to target various disease type based on patient’s specific biomarkers or genetic mutation ChemAladdin offers broad range of building blocks to enable the construction of interesting new molecules. Below we are showcasing selected examples of quinoxaline derivatives in context of our highlighted molecule. For more, please visit https://www.chemaladdin.com/ to register and search from millions of building blocks, screening compounds and reaction intermediates.

 

[1] Tariq S.; Somakala, K.; Amir, M. Eur. J. Med. Chem. 2018, 143, 542–557

[2] https://www.fda.gov/news-events/press-announcements/fda-approves-first-targeted-therapy-metastatic-bladder-cancer

[3] https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100375/balversa-erdafitinib 

Highlight #1: Egaten (Triclabendazole)

Apart from antiulcer and anthelmintic agents, benzamidazole derivatives are known for pharmacological activities e.g. anti-inflammatory, analgesic, antimicrobial, antiviral and anticancer indications.[i] In February 2019, FDA approved Egaten (Triclabendazole), a benzimidazole derivative, for treatment of patients with fascioliasis to Novartis.[ii] According to an estimation by World Health Organization (WHO) around 2.4 million people are infected with this disease[iii] and currently, Egaten is the only treatment recommended by the organization.[iv] A trial conducted in Vietnam on 100 patients with acute symptomatic fascioliasis randomized in two groups of 50 people each in order to compare the efficacy of triclabendazole to artesunate. Three months after the treatment, significantly high number of patients treated with triclabendazole reported no clinical symptoms of the disease as compared to later (92% vs 76%).[ii]

ChemAladdin offers numerous benzimidazole building blocks that can be employed for further derivatization or testing (below we are showcasing selected examples). For more, please visit https://www.chemaladdin.com/ to register and search from millions of building blocks, screening compounds and reaction intermediates.

ChemAladdin-Molecule-Week3

[i] Salahuddin; Shaharyar, M.; Mazumder, A. Arab. J. Chem. 2017, 10, S157–S173

[ii]https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100355/egaten-triclabendazole

[iii] Anonymus (1995). Control of Foodborne Trematode Infections. WHO Technical Series No. 849. WHO, Geneva, 157 pp

[iv]https://www.novartis.com/news/media-releases/novartis-receives-fda-approval-egaten-treatment-fascioliasis-neglected-tropical-disease

Molecule of the Week #2: Vizimpro® (Dacomitinib)

Quinazoline is a bicyclic aromatic heterocycle bearing two fused rings, a benzene ring and a pyrimidine ring. Quinazoline containing compounds are known for their antimalarial, anticancer, analgesic, antimicrobial, antihypertensive, anticonvulsant, and anti-tubercular activities.[i] Pfizer received approval from FDA in September 2018 for Vizimpro® (dacomitinib) to treat patients with metastatic non-small cell lung cancer with epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations.[ii] A comparative study on safety and efficacy of dacomitinib with Iressa (gefitinib, AstraZeneca) found the significant improvement in median progression-free survival duration of former (14.7 months compared to 9.2 months).[iii] Also, median overall survival with dacomitinib was 34.1 months as compared to 26.8 months for gefitinib.[iv]

Criteria

Vizimpro (Sep 2018)

Iressa (May 2013)

Median Overall Survival

34.1 months

26.8 months

Median Progression-free Survival

14.7 months

9.2 months

 

Both molecules have quinazoline heterocycle in their core structure and differ only in the substituent at C-6 of the quinazoline ring (see structures below).

Molecules in Week 2

It is interesting to note how small differences in functionalities can lead to such a positive outcome on patient’s lives. ChemAladdin offers a numbers of quinazoline derivatives that can be exploited for further derivatization or testing. Some examples of quinazoline building blocks that are available at ChemAladdin are shown above. For more, please visit https://www.chemaladdin.com to register and search from millions of building blocks, screening compounds and reaction intermediates.

[i] Gupta T.; Rohilla, A.; Pathak, A.; Akhtar, M. J.; Haider, M. R.; Yar M. S. Synth. Comm. 2018, 48, 1099–1127

[ii] https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100279/vizimpro-dacomitinib

[iii] Wu, Y.-L. and co-workers Lancet Oncol. 2017, 18, 1454–1466

[iv] http://www.ascopost.com/News/58920

Molecule of the Week #1: Xospata (Gilteritinib)

Pyrazines are six-membered heterocyclic aromatic compounds containing two nitrogen atoms in 1,4 positions. Pyrazine core is present in biological active compounds with antibiotic, anticancer and diuretic activities.[i] FDA approved pyridazine ring containing Xospata (gilteritinib) developed by Astellas Pharma to treat patients who have relapsed or refractory acute myeloid leukemia (AML) in November, 2018.[ii]

Some examples of pyrazine building blocks that are available at ChemAladdin are shown below. For more, please visit https://www.chemaladdin.com/ to register and search from millions of building blocks, screening compounds and reaction intermediates.

Molecule of the Week 1: Xospata (Gilteritinib)

[i] Dolezal, M.; Zitko, J. Expert Opinion on Therapeutic Patents, 2015, 33-47

[ii] https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100291/xospata-gilteritinib-