Page last updated: 2024-12-11

ckd732

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

CKD732: angiogenesis inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID74332265
MeSH IDM0469601

Synonyms (3)

Synonym
ckd732
[(3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] (e)-3-[4-[2-(dimethylamino)ethoxy]phenyl]prop-2-enoate
FT-0699345

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Sleep disturbance and gastrointestinal adverse events were more common with beloranib than with placebo; these were generally mild to moderate, transient and dose-related, and led to more early study withdrawals in participants in the group with the highest dose of beloranib."( Efficacy and safety of beloranib for weight loss in obese adults: a randomized controlled trial.
de Looze, F; Hughes, TE; Kim, DD; Krishnarajah, J; Lillioja, S; Marjason, J; Proietto, J; Shakib, S; Stuckey, BGA; Vath, JE, 2015
)
0.42
"4 mg dose was associated with increased sleep latency and mild to moderate gastrointestinal adverse events over the first month of treatment."( Efficacy and safety of beloranib for weight loss in obese adults: a randomized controlled trial.
de Looze, F; Hughes, TE; Kim, DD; Krishnarajah, J; Lillioja, S; Marjason, J; Proietto, J; Shakib, S; Stuckey, BGA; Vath, JE, 2015
)
0.42
" Beloranib, a MetAP2 inhibitor previously investigated for treatment of Prader-Willi syndrome, was associated with venous thrombotic adverse events likely resulting from drug effects on vascular endothelial cells (ECs)."( Preclinical Efficacy and Safety of the Novel Antidiabetic, Antiobesity MetAP2 Inhibitor ZGN-1061.
Burkey, BF; Hoglen, NC; Hughes, TE; Inskeep, P; Vath, JE; Wyman, M, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
"We conducted a Phase I clinical trial to evaluate the safety, tolerability, and pharmacokinetics (PK) of CKD-732 [6-O-(4-dimethylaminoethoxy) cinnamoyl fumagillol hemioxalate] in combination with capecitabine and oxaliplatin (XELOX) in nine metastatic colorectal cancer patients who had progressed on irinotecan-based chemotherapy."( A Phase Ib pharmacokinetic study of the anti-angiogenic agent CKD-732 used in combination with capecitabine and oxaliplatin (XELOX) in metastatic colorectal cancer patients who progressed on irinotecan-based chemotherapy.
Ahn, JB; Chung, HC; Hong, YS; Kim, C; Kim, DH; Kim, HR; Kim, TW; Lee, YJ; Park, KS; Rha, SY; Roh, JK; Shin, SJ, 2012
)
0.38
" The maximum tolerated dose was 10 mg/m(2)/d, and the clinically recommended dose was 5 mg/m(2)/d for CKD-732 in combination with XELOX."( A Phase Ib pharmacokinetic study of the anti-angiogenic agent CKD-732 used in combination with capecitabine and oxaliplatin (XELOX) in metastatic colorectal cancer patients who progressed on irinotecan-based chemotherapy.
Ahn, JB; Chung, HC; Hong, YS; Kim, C; Kim, DH; Kim, HR; Kim, TW; Lee, YJ; Park, KS; Rha, SY; Roh, JK; Shin, SJ, 2012
)
0.38
"The Phase II recommended dose of CKD-732 was determined to be 5 mg/m(2)/d, and this dose was safely combined with a conventional dose of capecitabine and oxaliplatin in this patient population."( A Phase Ib pharmacokinetic study of the anti-angiogenic agent CKD-732 used in combination with capecitabine and oxaliplatin (XELOX) in metastatic colorectal cancer patients who progressed on irinotecan-based chemotherapy.
Ahn, JB; Chung, HC; Hong, YS; Kim, C; Kim, DH; Kim, HR; Kim, TW; Lee, YJ; Park, KS; Rha, SY; Roh, JK; Shin, SJ, 2012
)
0.38

Dosage Studied

ExcerptRelevanceReference
" CKD-732 was intravenously administered with the dosages of 10, 30, 40 or 50 mg/kg and the highest dosage of 50 mg/kg prolonged the hexobarbital-induced sleep time."( General pharmacology of CKD-732, a new anticancer agent: effects on central nervous, cardiovascular, and respiratory system.
Kim, EJ; Shin, WH, 2005
)
0.33
" Dosing was stopped early due to an imbalance in venous thrombotic events in beloranib-treated participants (2 fatal events of pulmonary embolism and 2 events of deep vein thrombosis) compared with placebo."( Effects of MetAP2 inhibition on hyperphagia and body weight in Prader-Willi syndrome: A randomized, double-blind, placebo-controlled trial.
Abuzzahab, MJ; Angulo, M; Barlow, SE; Bird, LM; Butler, MG; Chan, CL; Dykens, EM; Fu, C; Hughes, TE; Kim, DD; Malloy, J; McCandless, SE; Miller, J; Myers, SE; Roof, E; Salehi, P; Scheimann, AO; Stafford, D; Styne, D; Taylor, K; Viskochil, D; Whitman, BY; Yanovski, JA; Zhuang, D, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (31.58)29.6817
2010's12 (63.16)24.3611
2020's1 (5.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (31.58%)5.53%
Reviews4 (21.05%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (47.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 1b Trial of Beloranib, a Novel Methionine Aminopeptidase 2 (MetAP-2) Inhibitor for Treatment of Extreme Obesity: Randomized, Double-Blind, Placebo-Controlled, Escalating Doses in Female Volunteers [NCT01372761]Phase 125 participants (Actual)Interventional2011-06-30Completed
Randomized, Double-Blind, Placebo Controlled, Phase 3 Trial of ZGN-440 (Subcutaneous Beloranib in Suspension) in Obese Subjects With Prader-Willi Syndrome to Evaluate Total Body Weight, Food-related Behavior, and Safety Over 6 Months [NCT02179151]Phase 3108 participants (Actual)Interventional2014-09-30Terminated(stopped due to FDA Clinical Hold)
A Randomized, Double-Blind, Placebo-Controlled Multiple Dose Study, to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ZGN-433 in Obese Volunteers [NCT01028261]Phase 131 participants (Actual)Interventional2009-12-31Completed
Randomized, Double-Blind, Placebo Controlled, Phase 2a Trial of ZGN-440 (Subcutaneous Beloranib in Suspension), A Novel Methionine Aminopeptidase 2 Inhibitor, in Obese Subjects With Hypothalamic Injury to Evaluate Weight Reduction and Safety Over 4 Weeks [NCT02063295]Phase 214 participants (Actual)Interventional2014-04-30Completed
Randomized, Double-Blind, Placebo Controlled, Parallel Dose Ranging Phase 2a Trial of ZGN-440 (Subcutaneous Beloranib in Suspension), A Novel Methionine Aminopeptidase 2 Inhibitor, in Over-weight and Obese Subjects With Prader-Willi Syndrome to Evaluate W [NCT01818921]Phase 217 participants (Actual)Interventional2013-06-30Completed
ZGN-440 (Beloranib for Subcutaneous Injection), A Novel Methionine Aminopeptidase 2 Inhibitor for Treatment of Obesity: A Randomized Double-Blind Placebo Controlled Dose Escalation Phase 1b Trial to Evaluate Safety, Pharmacokinetics, Pharmacodynamics and [NCT01507077]Phase 125 participants (Actual)Interventional2011-12-31Completed
Randomized, Double-Blind, Placebo Controlled, Dose Ranging Phase 2 Trial of Beloranib (ZGN-440 for Injectable Suspension), A Novel Methionine Aminopeptidase 2 Inhibitor, in Obese Subjects to Evaluate Weight Reduction, Safety, and Pharmacokinetics Over 12 [NCT01666691]Phase 2160 participants (Actual)Interventional2012-08-31Completed
Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of ZGN-440 (Subcutaneous Beloranib in Suspension) in Obese Subjects With Type 2 Diabetes Mellitus to Evaluate Weight Reduction, Glycemic Control, Safety, and Tolerability [NCT02324491]Phase 2152 participants (Actual)Interventional2014-12-31Terminated(stopped due to Sponsor decision to analyze available safety and efficacy data)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]