Umbralisib: First Approval

Dhillon, Sohita; Keam, Susan J.

doi:10.1007/s40265-021-01504-2

Cited by 51 publications

(28 citation statements)

References 17 publications

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“…Umbralisib was granted a priority review and approved for the treatment of marginal zone and follicular lymphoma patients who have previously received systemic therapy. Umbralisib is well tolerated (Dhillon and Keam 2021 ). Melphalan flufenamide (melflufen) is a derivative of melphalan, which was developed nearly 60 years ago and is still used for palliation in the therapy of multiple myeloma (Morabito et al 2021 ).…”

Section: Methodsmentioning

confidence: 99%

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2021

Kaykı-Mutlu

Aksoyalp

Wojnowski

et al. 2022

Naunyn-Schmiedeberg's Arch Pharmacol

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The second year of the COVID-19 pandemic had no adverse effect on the number of new drug approvals by the US Food and Drug Administration (FDA). Quite the contrary, with a total of 50 new drugs, 2021 belongs to the most successful FDA years. We assign these new drugs to one of three levels of innovation: (1) first drug against a condition (“first-in-indication”), (2) first drug using a novel molecular mechanism (“first-in-class”), and (3) “next-in-class”, i.e., a drug using an already exploited molecular mechanism. We identify 21 first-in-class, 28 next-in-class, and only one first-in-indication drugs. By treatment area, the largest group is once again cancer drugs, many of which target specific genetic alterations. Every second drug approved in 2021 targets an orphan disease, half of them being cancers. Small molecules continue to dominate new drug approvals, followed by antibodies and non-antibody biopharmaceuticals. In 2021, the FDA continued to approve drugs without strong evidence of clinical effects, best exemplified by the aducanumab controversy.

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Section: Methodsmentioning

confidence: 99%

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2021

Kaykı-Mutlu

Aksoyalp

Wojnowski

et al. 2022

Naunyn-Schmiedeberg's Arch Pharmacol

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“…[ 73 ] Subsequently, in 2017, the pan-I PI3K inhibitor copanlisib (Bayer) [ 74 ] and the dual PI3Kδ/PI3Kγ inhibitor duvelisib (Verastem) [ 75 ] were approved in 2017. PI3Kα inhibitor alpelisib (Novartis) [ 76 ] was approved for the treatment of advanced breast cancer in 2019 and umbralisib (TG Therapeutics) [ 77 ] for the treatment of chronic lymphocytic leukemia, follicular lymphoma, and marginal zone lymphoma in 2021 has also been approved for listing. In addition to these PI3K inhibitors approved by the FDA for clinical treatment, there are several new PI3K inhibitors for NSCLC in various experimental stages.…”

Section: Research Of Pi3k Inhibitors In Nsclcmentioning

confidence: 99%

Treating non-small cell lung cancer by targeting the PI3K signaling pathway

Jiang

Zhang

et al. 2022

Chinese Medical Journal

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The phosphosphatidylinositol-3-kinase (PI3K) signaling pathway is one of the most important intracellular signal transduction pathways affecting cell functions, such as apoptosis, translation, metabolism, and angiogenesis. Lung cancer is a malignant tumor with the highest morbidity and mortality rates in the world. It can be divided into two groups, non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC). NSCLC accounts for >85% of all lung cancers. There are currently many clinical treatment options for NSCLC; however, traditional methods such as surgery, chemotherapy, and radiotherapy have not been able to provide patients with good survival benefits. The emergence of molecular target therapy has improved the survival and prognosis of patients with NSCLC. In recent years, there have been an increasing number of studies on NSCLC and PI3K signaling pathways. Inhibitors of various parts of the PI3K pathway have appeared in various phases of clinical trials with NSCLC as an indication. This article focuses on the role of the PI3K signaling pathway in the occurrence and development of NSCLC and summarizes the current clinical research progress and possible development strategies.

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“…Tepotinib hydrochloride hydrate is claimed explicitly in US8329692B2 [201]. Umbralisibtosylate (Figure 69) is a chromen-4-one based pyrazolo [3,4-d]pyrimidine derivative (MF: C38H32F3N5O6S; 743.75; 1532533-72-4) [202]. US10570142B2 provides pyrazolo [3,4-d]pyrimidines as inhibitors of PI3Kδ and their pharmaceutical compositions to treat PI3Kδ mediated disorders.…”

Section: Tepotinib Hydrochloride Monohydratementioning

confidence: 99%

Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

Imran

Asdaq²,

Khan³

et al. 2021

Pharmaceuticals

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Protein kinase inhibitors (PKIs) are important therapeutic agents. As of 31 May 2021, the United States Food and Drug Administration (USFDA) has approved 70 PKIs. Most of the PKIs are employed to treat cancer and inflammatory diseases. Imatinib was the first PKI approved by USFDA in 2001. This review summarizes the compound patents and the essential polymorph patents of the PKIs approved by the USFDA from 2001 to 31 May 2021. The dates on the generic drug availability of the PKIs in the USA market have also been forecasted. It is expected that 19 and 48 PKIs will be genericized by 2025 and 2030, respectively, due to their compound patent expiry. This may reduce the financial toxicity associated with the existing PKIs. There are nearly 535 reported PKs. However, the USFDA approved PKIs target only about 10–15% of the total said PKs. As a result, there are still a large number of unexplored PKs. As the field advances during the next 20 years, one can anticipate that PKIs with many scaffolds, chemotypes, and pharmacophores will be developed.

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Umbralisib: First Approval

Cited by 51 publications

References 17 publications

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2021

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2021

Treating non-small cell lung cancer by targeting the PI3K signaling pathway

Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

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