Delving into the Latest Updates on Ezetimibe/Pitavastatin Calcium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pitavastatin Calcium Hydrate/Ezetimibe, 依折麦布/匹伐他汀钙

+ [6]

Target

CETP x HMGCR

Action

inhibitors

Mechanism

CETP inhibitors(Cholesteryl ester transfer protein inhibitors), HMG-CoA reductase inhibitors(HMG-CoA reductase inhibitors)

Therapeutic Areas

Congenital DisordersEndocrinology and Metabolic Disease

Active Indication

HypercholesterolemiaHyperlipoproteinemia Type IIPrimary hypercholesterolemia

Inactive Indication

Homozygous familial hypercholesterolemia

Originator Organization

Kowa Co., Ltd.

Active Organization

Kowa Co., Ltd.

JW PHARMACEUTICAL Corp.

Addpharma, Inc.

+ [1]

Inactive Organization

Lepu Pharmaceutical Technology Co., Ltd.

License Organization-

Drug Highest PhaseApproved

First Approval Date

South Korea (28 Jul 2021),

Primary hypercholesterolemia

Regulation-

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Structure/Sequence

Molecular FormulaC24H21F2NO3

InChIKeyOLNTVTPDXPETLC-XPWALMASSA-N

CAS Registry163222-33-1

View All Structures (2)

AIMEzetimibe administration with ongoing statin therapy is an effective option for further lowering low-density lipoprotein cholesterol (LDL-C) levels. Thus, we investigated the long-term efficacy and safety of fixed-dose combination of pitavastatin/ezetimibe (K-924 LD: 2 mg/10 mg; K-924 HD: 4 mg/10 mg).METHODSWe conducted a phase III, multicenter, open-label trial involving patients with hypercholesterolemia receiving pitavastatin (2 or 4 mg) who had not achieved their LDL-C management target. Patients were enrolled into the K-924 LD and HD groups based on whether they had received pitavastatin 2 and 4 mg, respectively, and treated for 52 weeks. K-924 was administered orally once daily. The primary objective was to examine the percent change in LDL-C from baseline at week 52 with last observation carried forward imputation (LOCF) in all patients.RESULTSOf the 109 patients evaluated, 62 and 47 were assigned to the K-924 LD and HD groups, respectively. In all patients, LDL-C decreased by -30.3±14.3% (p＜0.001) from baseline (134.4±37.9 mg/dL). Consequently, 91.8% and 37.5% of the patients for primary and secondary prevention reached their LDL-C management target, respectively. These results were consistent in both the K-924 LD and HD groups. In the safety analysis, a single adverse drug reaction occurred in a patient in the K-924 HD group.CONCLUSIONAfter replacing pitavastatin monotherapy, K-924 was found to be effective and well-tolerated over 52 weeks. Thus, K-924 can contribute to intensifying LDL-C-lowering therapy without increasing the number of medications.

01 Nov 2023·Journal of Atherosclerosis and Thrombosis

Efficacy and Safety of Pitavastatin/Ezetimibe Fixed-Dose Combination vs. Pitavastatin: Phase III, Double-Blind, Randomized Controlled Trial

Article

Author: Ako, Junya ; Suganami, Hideki ; Yokote, Koutaro ; Tanigawa, Ryohei ; Tajima, Sachiko ; Tsujita, Kenichi

AIMWe compared the efficacy and safety of pitavastatin/ezetimibe fixed-dose combination with those of pitavastatin monotherapy in patients with hypercholesterolemia.METHODSThis trial was a multicenter, randomized, double-blind, active-controlled, parallel-group trial. A total of 293 patients were randomly assigned into four groups receiving 2 mg pitavastatin, 4 mg pitavastatin, 2 mg pitavastatin/10 mg ezetimibe (K-924 LD), and 4 mg pitavastatin/10 mg ezetimibe (K-924 HD) once daily for 12 weeks.RESULTSThe percentage changes in low-density lipoprotein cholesterol (LDL-C), the primary endpoint, were -39.5% for 2 mg pitavastatin, -45.2% for 4 mg pitavastatin, -51.4% for K-924 LD, and -57.8% for K-924 HD. Compared with pitavastatin monotherapy, the pitavastatin/ezetimibe fixed-dose combination significantly reduced LDL-C, total cholesterol, and non-high-density lipoprotein cholesterol. Meanwhile, the cholesterol synthesis marker, lathosterol, was significantly decreased with pitavastatin monotherapy and the pitavastatin/ezetimibe fixed-dose combination, although the decrease was attenuated in the latter. On the other hand, the cholesterol absorption markers, beta-sitosterol and campesterol, were reduced with the fixed-dose combination but not with pitavastatin monotherapy. The incidence of adverse events and adverse drug reactions was not significantly different between the two groups receiving the fixed-dose combination and monotherapy. The mean values of laboratory tests that are related to liver function and myopathy increased but remained within the reference range in all groups.CONCLUSIONSThe pitavastatin/ezetimibe fixed-dose combination showed an excellent LDL-C-reducing effect by the complementary pharmacological action of each component, and its safety profile was similar to that of pitavastatin monotherapy (ClinicalTrials.gov Identifier: NCT04289649).

100 Deals associated with Ezetimibe/Pitavastatin Calcium

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypercholesterolemia	Japan	Kowa Co., Ltd.	26 Sep 2022
Hyperlipoproteinemia Type II	Japan	Kowa Co., Ltd.	26 Sep 2022
Primary hypercholesterolemia	South Korea	JW PHARMACEUTICAL Corp.	28 Jul 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypercholesterolemia	IND Approval	China	Zhejiang Lepu Pharmaceutical Co., Ltd.	20 Apr 2022
Homozygous familial hypercholesterolemia	Discovery	China	Lepu Pharmaceutical Technology Co., Ltd.	20 Sep 2022
Primary hypercholesterolemia	Discovery	China	Lepu Pharmaceutical Technology Co., Ltd.	20 Sep 2022