Biomaterial Database

Pharmacology of Pimasertib, A Selective MEK1/2 Inhibitor. 2018

Nuggehally R Srinivas

Zydus Research Centre, Ahmedabad, Gujarat, 382210, India. nuggehally.srinivas@zyduscadila.com.

Pimasertib belongs to the growing family of mitogen activated protein kinase (MEK1/2) inhibitors undergoing clinical development for various cancer indications. Since the MEK inhibition in several cell signalling transduction cascades within tumours was considered therapeutically beneficial, number of clinical investigations of pimasertib have been reported. Despite being orally bioavailable in cancer patients, pimasertib undergoes faster clearance with a short elimination half-life. In addition, due to occurrence of toxicity, the development of pimasertib appears to be stalled. Case studies are provided on the possible utilization of pimasertib in combination therapies with other approved drugs. Based on the review, it appeared that there was the need to identify the optimal dose and the dosing regimen of pimasertib to provide a balance between safety and efficacy when combined with approved therapies.

UI	MeSH Term	Description	Entries
D009369	Neoplasms	New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	Benign Neoplasm,Cancer,Malignant Neoplasm,Tumor,Tumors,Benign Neoplasms,Malignancy,Malignant Neoplasms,Neoplasia,Neoplasm,Neoplasms, Benign,Cancers,Malignancies,Neoplasias,Neoplasm, Benign,Neoplasm, Malignant,Neoplasms, Malignant
D009536	Niacinamide	An important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and/or cure of blacktongue and PELLAGRA. Most animals cannot manufacture this compound in amounts sufficient to prevent nutritional deficiency and it therefore must be supplemented through dietary intake.	Nicotinamide,Vitamin B 3,Vitamin PP,3-Pyridinecarboxamide,Enduramide,Nicobion,Nicotinsäureamid Jenapharm,Papulex,Vitamin B3,3 Pyridinecarboxamide,B 3, Vitamin,B3, Vitamin,Jenapharm, Nicotinsäureamid
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D047428	Protein Kinase Inhibitors	Agents that inhibit PROTEIN KINASES.	Protein Kinase Inhibitor,Inhibitor, Protein Kinase,Inhibitors, Protein Kinase,Kinase Inhibitor, Protein,Kinase Inhibitors, Protein
D048369	MAP Kinase Kinase 1	An abundant 43-kDa mitogen-activated protein kinase kinase subtype with specificity for MITOGEN-ACTIVATED PROTEIN KINASE 1 and MITOGEN-ACTIVATED PROTEIN KINASE 3.	MAP2K1 Protein,MAPK Kinase 1,MEK-1 Protein Kinase,MEK1 Protein Kinase,MKK-1 Protein Kinase,MKK1 Protein Kinase,Mitogen-Activated Protein Kinase Kinase 1,MEK 1 Protein Kinase,MKK 1 Protein Kinase,Mitogen Activated Protein Kinase Kinase 1
D048370	MAP Kinase Kinase 2	A 44 kDa mitogen-activated protein kinase kinase with specificity for MITOGEN-ACTIVATED PROTEIN KINASE 1 and MITOGEN-ACTIVATED PROTEIN KINASE 3.	Kinase Activator Kinase MEK2,MAP2K2 Protein,MAPK Extracellular Signal-Regulated Kinase 2,MAPK Kinase 2,MAPK-ERK Kinase 2,MEK-2 (MAPK Extracellular Signal-Regulated Kinase 2),MEK2 (MAPK Extracellular Signal-Regulated Kinase 2),Mitogen-Activated Protein Kinase Kinase 2,MAPK ERK Kinase 2,MAPK Extracellular Signal Regulated Kinase 2,Mitogen Activated Protein Kinase Kinase 2