The purpose of this trial is to study MK0731 in patients with recurrent or non-responsive solid tumors, or cancers for which standard therapy does not exist.
This is an early phase trial and some specific protocol information is proprietary and not publicly available at this time. (Full information is available to trial participants).

Start Date01 May 2005

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

100 Clinical Results associated with MK-0731

100 Translational Medicine associated with MK-0731

100 Patents (Medical) associated with MK-0731

Literatures (Medical) associated with MK-0731

01 Jun 2024·Archives of Biochemistry and Biophysics

Binding patterns of inhibitors to different pockets of kinesin Eg5

Article

Author: Geng, Yizhao ; Huo, Ziling ; Jia, Ning ; Ji, Qing ; Zhang, Bingbing ; Qin, Jingyu

The kinesin-5 family member, Eg5, plays very important role in the mitosis. As a mitotic protein, Eg5 is the target of various mitotic inhibitors. There are two targeting pockets in the motor domain of Eg5, which locates in the α2/L5/α3 region and the α4/α6 region respectively. We investigated the interactions between the different inhibitors and the two binding pockets of Eg5 by using all-atom molecular dynamics method. Combined the conformational analysis with the free-energy calculation, the binding patterns of inhibitors to the two binding pockets are shown. The α2/L5/α3 pocket can be divided into 4 regions. The structures and binding conformations of inhibitors in region 1 and 2 are highly conserved. The shape of α4/α6 pocket is alterable. The space of this pocket in ADP-binding state of Eg5 is larger than that in ADP·Pi-binding state due to the limitation of a hydrogen bond formed in the ADP·Pi-binding state. The results of this investigation provide the structural basis of the inhibitor-Eg5 interaction and offer a reference for the Eg5-targeted drug design.

26 Jan 2018·Chemistry – A European JournalQ2 · CHEMISTRY

Cobalt‐Catalyzed Asymmetric Allylation of Cyclic Ketimines

Q2 · CHEMISTRY

Article

Author: Wu, Liang ; Yang, Guoqiang ; Zhang, Wanbin ; Shao, Qihang

AbstractA CoII/Box‐catalyzed [Box=bis(oxazoline)] enantioselective addition of potassium allyltrifluoroborate to cyclic ketimines was developed, providing the corresponding chiral α‐tertiary amines in high yields and with good enantioselectivity values. Alkoxycarbonyl‐ and alkyl‐substituted saccharin‐derived ketimines are suitable substrates for this allylation reaction. The product can be converted to complex molecules over several simple steps, including a precursor of MK‐0371, which is a kinesin spindle protein inhibitor. In addition, this catalytic system showed a strong positive nonlinear effect.

01 May 2015·Bioorganic & Medicinal ChemistryQ3 · MEDICINE

Discovery of novel spiro 1,3,4-thiadiazolines as potent, orally bioavailable and brain penetrant KSP inhibitors

Q3 · MEDICINE

Article

Author: Liu, Ming ; Siddiqui, M Arshad ; Basso, Andrea D ; Tang, Huadong ; Vitharana, Dilrukshi ; Allbritton, Omaira ; Dai, Chaoyang ; Angeles, Angie R ; Yang, Liping ; Mansoor, Umar Faruk ; Gray, Kimberly ; Liang, Lianzhu

Kinesin spindle protein (KSP) is a mitotic kinesin that is expressed only in proliferating cells and plays a key role in spindle pole separation, formation of a bipolar mitotic spindle, as well as centrosome separation and maturation. Inhibition of KSP has the potential to provide anti-tumor activity while avoiding peripheral neuropathy associated with some microtubule-targeted drugs. Based on MK-0731 and related heterocyclic compounds targeting the KSP monastrol binding site, structurally constrained spiro-cyclic KSP inhibitors were designed. In particular, rapid evaluation and optimization of the novel spiro 1,3,4-thiadiazolines resulted in a series of potent KSP inhibitors demonstrating mechanism based activities in cells, including induction of the mitotic marker phospho-histone H3 and induction of monaster spindle formation. Further optimization of the pharmacokinetic (PK) properties afforded MK-8267 as a potent, orally bioavailable and brain penetrant KSP inhibitor which showed anti-tumor activity in preclinical xenograft models.

100 Deals associated with MK-0731

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB08037

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 1	-	Merck Sharp & Dohme Corp.	01 May 2005
Solid tumor	Phase 1	United States	Merck GmbH	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00104364 (Pubmed \| Invest New Drugs)	Phase 1	Solid tumor	30	MK-0731	(efkcpojsbb) = weuxrpibbr vykvctgmjk (hlrzfkjdsu, ±7.3) View more	-	01 Jun 2012
ASCO2007	Phase 1	Solid tumor	35	MK-0731	(jckpxcubho) = jgxomxwdxn ocvgpmvfto (amuwvacfqa ) View more	-	20 Jun 2007
ASCO2006	Phase 1	Neoplasms	8	MK-0731	(pygoijesdf) = was observed in 2 pts at 48 mg/m2/24 hrs leading to expansion of cohorts at lower dose levels znpeccouil (xxyqxurbvc )	-	20 Jun 2006

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