Pacritinib for the treatment of patients with myelofibrosis and thrombocytopenia

Mascarenhas, John

doi:10.1080/17474086.2022.2112565

Cited by 34 publications

(16 citation statements)

References 84 publications

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“…Myelofibrosis is a rare myeloproliferative neoplasm; myelofibrosis patients have an augmented activation of Janus kinase signaling, which leads to severe thrombocytopenia with a poor prognosis (Patel and Odenike 2020 ; Mascarenhas 2022 ). Pacritinib is a small-molecule, highly selective inhibitor of Janus kinase-2/interleukin-1 receptor-associated kinase 1 (Singer et al 2016 ) that decreased the splenomegaly and improved symptoms in myelofibrosis patients (Mascarenhas 2022 ). Pacritinib has been approved for intermediate or high-risk myelofibrosis with a thrombocyte level < 50 × 10 9 /L.…”

Section: Oncologymentioning

confidence: 99%

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

Kaykı-Mutlu

Aksoyalp

Wojnowski

et al. 2023

Naunyn-Schmiedeberg's Arch Pharmacol

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While new drug approvals by the U.S. Food and Drug Administration (FDA) had remained stable or even increased in the first 2 years of the COVID-19 pandemic, the 37 newly approved drugs in 2022 are considerably less than the 53 and 50 new drugs approved in 2020 and 2021, respectively, and less than the rolling 10-year average of 43. As in previous years of this annual review, we assign these new drugs to one of three levels of innovation: first drug against a condition (“first-in-indication”), first drug using a novel molecular mechanism (“first-in-class”), and “next-in-class,” i.e., a drug using an already exploited molecular mechanism. We identify two “first-in-indication” (ganaxolon and teplizumab), 20 (54%) “first-in-class,” and 17 (46%) “next-in-class” drugs. By treatment area, rare diseases and cancer drugs were once again the most prevalent (partly overlapping) therapeutic areas. Other continuing trends were the use of accelerated regulatory approval pathways and the reliance on biopharmaceuticals (biologics).

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Section: Oncologymentioning

confidence: 99%

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

Kaykı-Mutlu

Aksoyalp

Wojnowski

et al. 2023

Naunyn-Schmiedeberg's Arch Pharmacol

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“…116 Pacritinib is a JAK2 inhibitor containing the benzene-pyrimidine biaryl and macrocyclic fragments, which could be used for the treatment of myelofibrosis through inhibiting the function of JAK2 and downstream JAK-STAT pathway. 117…”

Section: Oncologic Drugsmentioning

confidence: 99%

“…Olutasidenib is an isocitrate dehydrogenase‐1 (IDH1) inhibitor containing several amide fragments, which could be used for the treatment of AML through reducing the levels of 2‐hydroxyglutarate (2‐HG) 116 . Pacritinib is a JAK2 inhibitor containing the benzene‐pyrimidine biaryl and macrocyclic fragments, which could be used for the treatment of myelofibrosis through inhibiting the function of JAK2 and downstream JAK‐STAT pathway 117 …”

Section: Oncologic Drugsmentioning

confidence: 99%

New drug approvals for 2022: Synthesis and clinical applications

Yuan

Shen

Jia

et al. 2023

Medicinal Research Reviews

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The U.S. Food and Drug Administration has approved a total of 37 new drugs in 2022, which are composed of 20 chemical entities and 17 biologics. In particular, 20 chemical entities, including 17 small molecule drugs, 1 radiotherapy, and 2 diagnostic agents, provide privileged scaffolds, breakthrough clinical benefits, and a new mechanism of action for the discovery of more potent clinical candidates. The structure‐based drug development with clear targets and fragment‐based drug development with privileged scaffolds have always been the important modules in the field of drug discovery, which could easily bypass the patent protection and bring about improved biological activity. Therefore, we summarized the relevant valuable information about clinical application, mechanism of action, and chemical synthesis of 17 newly approved small molecule drugs in 2022. We hope this timely and comprehensive review could bring about creative and elegant inspiration on the synthetic methodologies and mechanism of action for the discovery of new drugs with novel chemical scaffolds and extended clinical indications.

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“…64 In 2022, the FDA approved pacritinib to treat patients with intermediate or high-risk or secondary MF and those with low platelet levels (Table 1). Additionally, the kinase profile of pacritinib showed it could inhibit the activity of Macrophage colony stimulating factor 1, Interleukin-1 receptor-associated kinase 1, 65 and FMS-like tyrosine kinase 3 (FLT3). 41 Therefore, pacritinib may also treat disease conditions such as acute myeloid leukemia (AML), myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), and chronic lymphocytic leukemia (CLL) besides MF.…”

Section: Macrocyclic Compounds That Inhibit Jak2mentioning

confidence: 99%

Applications of macrocyclic molecules in cancer therapy: Target cancer development or overcome drug resistance

Song,

Wu,

et al. 2023

MedComm – Oncology

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Cancer is a worldwide leading cause of cancer‐related death due to a lack of efficient disease control by drugs. With the increasing unmet needs in cancer treatment, developing novel effective cancer drugs is in great demand. Macrocyclic molecules represent a group of drug molecules with a cyclic skeleton which endows them with unique drug properties such as improved bioavailability, enhanced metabolic stability, increased binding affinity, and favorable pharmacokinetics parameters. The Food and Drug Administration (FDA) has approved a bunch of macrocyclic drugs to treat cancer patients. However, the importance of such molecules in cancer drug development remains underestimated. Recent studies support that macrocyclic molecules can also serve as an effective strategy to overcome drug resistance in cancer treatment, but is a lack of review. The purpose of this manuscript was to provide shreds of evidence on the applications of macrocyclic molecules for cancer therapy: (1) act as cancer drugs to target different proteins critical for cancer development; (2) act as cancer drugs to target resistant mutants of oncogenes to overcome drug resistance in targeted therapy. This review will help to attract more interest in developing macrocyclic drugs for cancer therapy and potentially provide more novel strategies to benefit cancer patients and society.

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Pacritinib for the treatment of patients with myelofibrosis and thrombocytopenia

Cited by 34 publications

References 84 publications

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

New drug approvals for 2022: Synthesis and clinical applications

Applications of macrocyclic molecules in cancer therapy: Target cancer development or overcome drug resistance

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