| Drug Name |
Selumetinib |
| Drug ID |
BADD_D02594 |
| Description |
Activation of the Raf-MEK-ERK signaling pathway is known to be implemented in several types of malignancies, thus, mitogen-activated protein kinase kinase (MEK) inhibitors such as selumetinib are important tools that can target the problematic overactivity of this pathway.[A193611]
Results from clinical trials investigating earlier developed MEK inhibitors were underwhelming.[A193611] However, selumetinib demonstrated impressive efficacy and tolerability in Phase I trials, leading to its continued investigation for the treatment of various types of tumors in Phase II trials.[A193611]
Currently, the novel MEK 1 / 2 inhibitor, selumetinib, is approved solely for the treatment of Neurofibromatosis type 1 (NF-1) in a limited age group. NF-1 is considered rare with an estimated incidence of 1/3000 individuals.[A193608] It is a genetic, autosomal dominant condition resulting from mutations of the NF1 gene, which can lead to various complications including the development of multiple tumors in the nervous system.[A193533,A193608] Some patients with this disorder develop plexiform neurofibromas (PN); however, this is considered to be relatively uncommon compared to other variants of NF-1.[A193608] Luckily, the use of selumetinib in patients with NF-1 has shown efficacy in shrinking associated tumors and is linked to other positive clinical outcomes.[A193533] |
| Indications and Usage |
Although selumetinib has been investigated for the treatment of several types of cancer, it is currently only indicated for the treatment of neurofibromatosis type 1 (NF1) in patients ≥2 years who have symptomatic, inoperable plexiform neurofibromas (PN).[A193611,L12852,L12969] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EE04 |
| DrugBank ID |
DB11689
|
| KEGG ID |
D09666
|
| MeSH ID |
C517975
|
| PubChem ID |
10127622
|
| TTD Drug ID |
D0T5DP
|
| NDC Product Code |
67651-0344; 0310-0610; 0310-0625; 67651-0343 |
| UNII |
6UH91I579U
|
| Synonyms |
AZD 6244 | AZD6244 | AZD-6244 | selumetinib | ARRY 142886 | ARRY142886 | ARRY-142886 |
