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DRUG CLASS:

ACVR1 inhibitor

2d
IKBKE modulates autophagy and progestin resistance in endometrial cancer. (PubMed, Front Oncol)
A progestin-resistant EC cell line was established to assess the effects of IKBKE knockdown and treatment with CYT387, a selective IKBKE inhibitor...These findings highlight the crucial role of IKBKE in regulating autophagy and mediating progestin resistance in EC. This study provides new insights into IKBKE as a potential molecular target that contributes to understanding the mechanisms underlying progestin resistance in endometrial cancer.
Journal
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IKBKE (Inhibitor Of Nuclear Factor Kappa B Kinase Subunit Epsilon)
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Ojjaara (momelotinib)
2d
A Study to Assess the Effectiveness and Safety of Pacritinib in Patients With VEXAS Syndrome (PAXIS) (clinicaltrials.gov)
P2, N=78, Active, not recruiting, Swedish Orphan Biovitrum | Recruiting --> Active, not recruiting
Enrollment closed
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Vonjo (pacritinib)
3d
Momelotinib in VEXAS Syndrome (clinicaltrials.gov)
P2, N=57, Recruiting, Groupe Francophone des Myelodysplasies | Not yet recruiting --> Recruiting
Enrollment open
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Ojjaara (momelotinib)
7d
To Assess the Efficacy, Safety, and Tolerability of INCB000928 in Participants With Fibrodysplasia Ossificans Progressiva (clinicaltrials.gov)
P2, N=98, Recruiting, Incyte Corporation | Trial primary completion date: Feb 2025 --> Jul 2027
Trial primary completion date
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zilurgisertib (INCB00928)
18d
Momelotinib Effectiveness in Myelofibrosis (clinicaltrials.gov)
P=N/A, N=93, Not yet recruiting, Gruppo Italiano Malattie EMatologiche dell'Adulto
New trial • Real-world evidence
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Ojjaara (momelotinib)
22d
Development of potent JAK1/2 PROTAC degraders for the treatment of inflammatory bowel diseases. (PubMed, Eur J Med Chem)
Herein, a novel series of PROTAC degraders based on momelotinib were designed and synthesised...Furthermore, in vivo studies demonstrated that A8 significantly reduced inflammatory responses and colon injury by suppressing the JAK/STAT3 signalling pathway. Overall, A8 represents a novel JAK1/2 degrader as a lead compound for IBD for the first time, which deserves further development.
Journal
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JAK2 (Janus kinase 2) • IL6 (Interleukin 6) • CRBN (Cereblon) • JAK1 (Janus Kinase 1)
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Ojjaara (momelotinib)
29d
Masking as Myelofibrosis: A Case of Tp53 Mutated Acute Erythroid Leukemia Presenting With Pancytopenia and Bone Pain. (PubMed, Case Rep Hematol)
He was started on JAK inhibitor therapy with pacritinib but clinically declined over the next several days with worsening diffuse pain and pancytopenia...Shortly after, the patient presented to an outside hospital with septic shock, at which point the patient expired. This case illustrates the aggressive nature of the disease, the need for confirmatory testing when diagnosis is suspected and the difficulty in management as the prognosis is poor and requires aggressive treatment that can lead to life-threatening sequelae.
Journal
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TP53 (Tumor protein P53) • JAK2 (Janus kinase 2)
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TP53 mutation
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Vonjo (pacritinib)
1m
Advancements in myelofibrosis management: a comprehensive analysis of Ojjaara (Momelotinib) therapy and clinical perspectives. (PubMed, Ann Med Surg (Lond))
This review examines the role of momelotinib in treating MF, focusing on its mechanism, clinical benefits, patient selection criteria, monitoring strategies, potential side effects, and findings from key clinical trials. While promising, careful patient management is essential to minimize adverse effects and optimize the therapeutic benefits of momelotinib in MF treatment.
Review • Journal
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JAK2 (Janus kinase 2) • JAK1 (Janus Kinase 1)
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Ojjaara (momelotinib)
2ms
Trial termination
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zilurgisertib (INCB00928)
2ms
Trial primary completion date
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ACVR1 (Activin A Receptor Type 1)