DDInter1628 DDInter9
Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2, which are tyrosine kinases involved in cytokine signalling and hematopoiesis. Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation. Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed. Rux
To date, acalabrutinib has been used in trials studying the treatment of B-All, myelofibrosis, ovarian cancer, multiple myeloma, and Hodgkin lymphoma, among others. As of October 31, 2017 the FDA approved Astra Zeneca's orally administered Calquence (acalabrutinib, capsules). This Bruton tyrosine kinase (BTK) inhibitor indicated for the treatment of chronic lymphocytic leukemia, small lymphocytic lymphoma, and in adult patients with Mantle cell lymphoma (MCL) who have already received at least one prior therapy. In August 2022, the FDA approved a new tablet formulation of Calquence, enabling the co-administration of this drug with proton pump inhibitors (PPIs).[L42795,L42800] Unlike Calquence capsules, the co-administration of Calquence tablets and PPIs does not have an effect in the pharmacokinetics of acalabrutinib.[L10241,L42795] Also known as ACP-196, acalabrutinib is also considered a second generation BTK inhibitor because it was rationally designed to be more potent and selective than ibrutinib, theoretically expected to demonstrate fewer adverse effects owing to minimized bystander effects on targets other than BTK. Nevertheless, acalabrutinib was approved under the FDA's accelerated approval pathway, which is based upon overall response rate and faciliates earlier approval of medicines that treat serious conditions or/and that fill an unmet medical need based on a surrogate endpoint. Continued approval for acalabrutinib's currently accepted indication may subsequently be contingent upon ongoing verification and description of clinical benefit in confimatory trials. Furthermore, the FDA granted this medication Priority Review and Breakthrough Therapy designations. It also received Orphan Drug designation, which provides incentives to assist and encourage the development of drugs for rare diseases. At this time, more than 35 clinical trials across 40 countries with more than 2500 patients are underway or have been completed with regards to further research into better understanding and expanding the therapeutic uses of acalabrutinib .
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Nilotinib
Nilotinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) BMP2K
BMP2K {u} (Gene) is bound by {v} (Compound) Crizotinib
Crizotinib {u} may lead to a major life threatening interaction when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) IRAK1
IRAK1 {u} (Gene) is downregulated by {v} (Compound) Omacetaxine mepesuccinate
Omacetaxine mepesuccinate {u} may lead to a major life threatening interaction when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Dasatinib
Dasatinib {u} may lead to a major life threatening interaction when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) STK16
STK16 {u} (Gene) is bound by {v} (Compound) Pazopanib
Pazopanib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK4
PLK4 {u} (Gene) is downregulated by {v} (Compound) Topotecan
Topotecan {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) CLK2
CLK2 {u} (Gene) is upregulated by {v} (Compound) Vemurafenib
Vemurafenib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK1
PLK1 {u} (Gene) is upregulated by {v} (Compound) Treprostinil
Treprostinil {u} may lead to a major life threatening interaction when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) upregulates {v} (Gene) FOXJ3
FOXJ3 {u} (Gene) is upregulated by {v} (Compound) Omacetaxine mepesuccinate
Omacetaxine mepesuccinate {u} may lead to a major life threatening interaction when taken with {v} Acalabrutinib
Ruxolitinib {u} (Compound) upregulates {v} (Gene) WAPAL
WAPAL {u} (Gene) is downregulated by {v} (Compound) Topotecan
Topotecan {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Acalabrutinib
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Nilotinib (Compound) and Nilotinib may cause a moderate interaction that could exacerbate diseases when taken with Acalabrutinib
Ruxolitinib (Compound) binds BMP2K (Gene) and BMP2K (Gene) is bound by Crizotinib (Compound) and Crizotinib may lead to a major life threatening interaction when taken with Acalabrutinib
Ruxolitinib (Compound) binds IRAK1 (Gene) and IRAK1 (Gene) is downregulated by Omacetaxine mepesuccinate (Compound) and Omacetaxine mepesuccinate may lead to a major life threatening interaction when taken with Acalabrutinib
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Dasatinib (Compound) and Dasatinib may lead to a major life threatening interaction when taken with Acalabrutinib
Ruxolitinib (Compound) binds STK16 (Gene) and STK16 (Gene) is bound by Pazopanib (Compound) and Pazopanib may cause a moderate interaction that could exacerbate diseases when taken with Acalabrutinib
Ruxolitinib (Compound) binds PLK4 (Gene) and PLK4 (Gene) is downregulated by Topotecan (Compound) and Topotecan may cause a moderate interaction that could exacerbate diseases when taken with Acalabrutinib
Ruxolitinib (Compound) binds CLK2 (Gene) and CLK2 (Gene) is upregulated by Vemurafenib (Compound) and Vemurafenib may cause a moderate interaction that could exacerbate diseases when taken with Acalabrutinib
Ruxolitinib (Compound) binds PLK1 (Gene) and PLK1 (Gene) is upregulated by Treprostinil (Compound) and Treprostinil may lead to a major life threatening interaction when taken with Acalabrutinib
Ruxolitinib (Compound) upregulates FOXJ3 (Gene) and FOXJ3 (Gene) is upregulated by Omacetaxine mepesuccinate (Compound) and Omacetaxine mepesuccinate may lead to a major life threatening interaction when taken with Acalabrutinib
Ruxolitinib (Compound) upregulates WAPAL (Gene) and WAPAL (Gene) is downregulated by Topotecan (Compound) and Topotecan may cause a moderate interaction that could exacerbate diseases when taken with Acalabrutinib