Chapter title |
Ruxolitinib
|
---|---|
Chapter number | 6 |
Book title |
Small Molecules in Hematology
|
Published in |
Recent results in cancer research Fortschritte der Krebsforschung Progrès dans les recherches sur le cancer, January 2018
|
DOI | 10.1007/978-3-319-91439-8_6 |
Pubmed ID | |
Book ISBNs |
978-3-31-991438-1, 978-3-31-991439-8
|
Authors |
Stefanie Ajayi, Heiko Becker, Heike Reinhardt, Monika Engelhardt, Robert Zeiser, Nikolas von Bubnoff, Ralph Wäsch, Ajayi, Stefanie, Becker, Heiko, Reinhardt, Heike, Engelhardt, Monika, Zeiser, Robert, von Bubnoff, Nikolas, Wäsch, Ralph |
Abstract |
Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of Janus kinase (JAK) 1 and JAK2. Ruxolitinib has been approved for the treatment of myelofibrosis (MF) by the US Food and Drug Administration (FDA) in 2011 and by the European Medicines Agency (EMA) in 2012, followed by the approval for the treatment of hydroxyurea (HU)-resistant or -intolerant polycythemia vera (PV) in 2014. Both MF and PV are myeloproliferative neoplasms (MPNs) which are characterized by the aberrant activation of the JAK-STAT pathway. Clinically, MF features bone marrow fibrosis, splenomegaly, abnormal blood counts, and poor quality-of-life through associated symptoms. PV is characterized by the overproduction of primarily red blood cells (RBC), risk of thrombotic complications, and development of secondary MF. Ruxolitinib treatment results in a meaningful reduction in spleen size and symptom burden in the majority of MF patients and may also have a favorable effect on survival. In PV, ruxolitinib effectively controls the hematocrit and reduces splenomegaly. Since recently, ruxolitinib is also under investigation for the treatment of graft-versus-host disease (GvHD) after allogeneic hematopoietic stem cell transplantation (HSCT). Toxicities of ruxolitinib include myelosuppression, which results in dose-limiting thrombocytopenia and anemia, and viral reactivations. The metabolization of ruxolitinib through CYP3A4 needs to be considered particularly if co-administered with potent CYP3A4 inhibitors. Several further JAK inhibitors are currently under investigation for MPNs or other immuno-inflammatory diseases. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 141 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Bachelor | 18 | 13% |
Student > Master | 13 | 9% |
Student > Ph. D. Student | 12 | 9% |
Student > Doctoral Student | 8 | 6% |
Other | 8 | 6% |
Other | 17 | 12% |
Unknown | 65 | 46% |
Readers by discipline | Count | As % |
---|---|---|
Medicine and Dentistry | 25 | 18% |
Biochemistry, Genetics and Molecular Biology | 21 | 15% |
Pharmacology, Toxicology and Pharmaceutical Science | 12 | 9% |
Agricultural and Biological Sciences | 6 | 4% |
Chemistry | 4 | 3% |
Other | 10 | 7% |
Unknown | 63 | 45% |