Delving into the Latest Updates on MDCO-216 with Synapse

Overview

Basic Info

Drug Type

Recombinant protein

Synonyms

AIM, ApoA1 Milano, r-ApoA-I Milano

+ [5]

Target

APOA1

Mechanism

APOA1 stimulants(Apolipoprotein A-I stimulants)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Acute Coronary SyndromeAtherosclerosisCoronary Artery Disease+ [1]

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

The Medicines Co.

Esperion Therapeutics, Inc.

Pfizer Inc.

+ [1]

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Sequence Code 13755

A multiple dose, dose-finding, placebo controlled, double blind, randomized trial to compare the effect of treatment on plaque burden as determined by intravascular ultrasound and evaluate the efficacy, safety, and tolerability of MDCO-216 given as multiple weekly infusions in subjects with a recent acute coronary syndrome event - MILANO DRIVE

Start Date26 Oct 2016

Sponsor / Collaborator

The Medicines Co.

EUCTR2015-000826-13-CZ

/ Not yet recruitingPhase 2

A placebo-controlled, double-blind, randomized trial to compare the effect of treatment on plaque burden as determined by intravascular ultrasound and to evaluate the efficacy, pharmacokinetics, safety, and tolerability of MDCO-216 given as multiple weekly infusions in subjects with a recent acute coronary syndrome. - MILANO PILOT

Start Date20 Jan 2016

Sponsor / Collaborator

The Medicines Co.

NCT02678923

/ CompletedPhase 1/2

A Placebo-controlled, Double-blind, Randomized Trial to Compare the Effect of Treatment on Plaque Burden as Determined by Intravascular Ultrasound and to Evaluate the Efficacy, Pharmacokinetics, Safety, and Tolerability of MDCO-216 Given as Multiple Weekly Infusions in Subjects With a Recent Acute Coronary Syndrome

This study will be a proof-of-concept, placebo-controlled, double-blind, randomized trial in participants with a recent acute coronary syndrome (ACS) to evaluate the efficacy, pharmacokinetics, safety, tolerability, disease progression measures by IVUS, and pharmacodynamics of MDCO-216 infusion. Eligible participants will be randomized to receive 5 infusions of MDCO-216 20 milligrams/kilogram (mg/kg) or placebo in a 1:1 ratio.

Start Date03 Dec 2015

Sponsor / Collaborator

The Medicines Co.

[+1]

100 Clinical Results associated with MDCO-216

Login to view more data

100 Translational Medicine associated with MDCO-216

Login to view more data

100 Patents (Medical) associated with MDCO-216

Login to view more data

85

Literatures (Medical) associated with MDCO-216

01 Feb 2025·Journal of Colloid and Interface Science

pH-responsive β-cyclodextrin-grafted chitosan microspheres: Dual-action smart carriers for enhanced corrosion inhibition

Article

Author: Cui, Nannan ; Wang, Zhikun ; Li, Miantuo ; Qu, Wentao ; Sun, Shuangqing ; Hu, Songqing ; Su, Huiling ; Li, Fengting

Micro/nanocontainers, as smart carriers of corrosion inhibitors, capable of intelligently detecting corroded areas and dispensing inhibitors precisely for targeted corrosion control. Here, pH-responsive chitosan-grafted-β-cyclodextrin (CS-g-β-CD) microspheres (CgCM) loaded with various corrosion inhibitors are prepared via an emulsification cross-linking method. By FT-IR and ¹H NMR characterizations, the successful loading of corrosion inhibitor BTA into β-CD is achieved, with the obtained BTA@β-CD being further grafted on the CS chain by degree 28.8 %. The prepared CgCM possess a size range from 15 to 20 μm, and a surface zeta potential range from positive in acidic solution (33.7 mV at pH = 3) to negative in alkaline solution (-20.4 mV at pH = 10). In addition to loading BTA into β-CD, three compound agents (AIM, AMIM-Cl, and 3-SAMA) are selected to be loaded into the crosslinking gaps of the CgCM, with the loading ratios of BTA, AIM, AMIM-Cl, and 3-SAMA determined to be 31.59 %, 13.85 %, 16.93 %, and 19.30 %, respectively. When subjected to acidic stimulation, the CgCM undergo swelling and dissociation, leading to the responsive release of the four loaded inhibitors into the solution, for which the accumulative release ratios (48 h, pH = 3) are determined to be 93 %, 86 %, 84 %, and 81 %, respectively. Weight loss and electrochemical evaluations firmly establish that these CgCM, laden with inhibitors, are adept at forming dense protective barriers on steel surfaces, achieving a corrosion inhibition efficiency exceeding 90 %. Corrosion morphology, surface elemental distribution, and binding status reveal a compact compounding protective layer formation on the steel/solution interface, by a physicochemical synergistic adsorption pattern. Density functional theory (DFT) calculations and molecular dynamics (MD) simulations reinforce the findings, revealing that all three CgCM systems exhibit targeted, stimulus-responsive release capabilities, coupled with robust adsorption strengths and remarkable corrosion resistance characteristics.

01 Apr 2024·Journal of Lipid Research

Apolipoprotein A1 and high-density lipoprotein limit low-density lipoprotein transcytosis by binding SR-B1

Article

Author: Xu, Zizhen ; Beauchemin, Catherine A A ; Fung, Karen Y Y ; Ho, Tse Wing Winnie ; Lee, Warren L ; Neculai, Dante ; Fairn, Gregory D

Atherosclerosis results from the deposition and oxidation of LDL and immune cell infiltration in the sub-arterial space leading to arterial occlusion. Studies have shown that transcytosis transports circulating LDL across endothelial cells lining blood vessels. LDL transcytosis is initiated by binding to either scavenger receptor B1 (SR-B1) or activin A receptor-like kinase 1 on the apical side of endothelial cells leading to its transit and release on the basolateral side. HDL is thought to partly protect individuals from atherosclerosis due to its ability to remove excess cholesterol and act as an antioxidant. Apolipoprotein A1 (APOA1), an HDL constituent, can bind to SR-B1, raising the possibility that APOA1/HDL can compete with LDL for SR-B1 binding, thereby limiting LDL deposition in the sub-arterial space. To examine this possibility, we used in vitro approaches to quantify the internalization and transcytosis of fluorescent LDL in coronary endothelial cells. Using microscale thermophoresis and affinity capture, we find that SR-B1 and APOA1 interact and that binding is enhanced when using the cardioprotective variant of APOA1 termed Milano (APOA1-Milano). In male mice, transiently increasing the levels of HDL reduced the acute deposition of fluorescently labeled LDL in the atheroprone inner curvature of the aorta. Reduced LDL deposition was also observed when increasing circulating wild-type APOA1 or the APOA1-Milano variant, with a more robust inhibition from the APOA1-Milano. The results suggest that HDL may limit SR-B1-mediated LDL transcytosis and deposition, adding to the mechanisms by which it can act as an atheroprotective particle.

01 Mar 2024·Journal of Cataract and Refractive Surgery

Anti-inflammatory medication use after cataract surgery: online survey of practice patterns

Article

Author: LaBorwit, Scott ; Riaz, Kamran M ; Woreta, Fasika A ; Prescott, Christina R ; Chang, David F ; Li, Ximin ; Zebardast, Nazlee ; Awidi, Abdelhalim A ; Daoud, Yassine J ; Srikumaran, Divya

Purpose:To determine current prescribing patterns for topical or intraocular/periocular anti-inflammatory medications (AIMs) after routine cataract surgery.Setting:kera-netonline members.Design:Cross-sectional survey.Methods:An online survey was distributed to subscribers ofkera-net, a global online platform sponsored by the Cornea Society. Questions were asked regarding the use of topical or intraocular/periocular AIM after cataract surgery and types of medications prescribed.Results:Of 217 surgeon respondents (23% response rate), 171 (79%) practiced in the United States and 171 (79%) were cornea subspecialists. Most of the respondents (n = 196, 97%) prescribed topical corticosteroids after routine cataract surgery. The most frequently prescribed were prednisolone acetate (n = 162, 83%), followed by dexamethasone (n = 26, 13%), difluprednate (n = 24, 12%), and loteprednol etabonate (n = 13, 7%). Corticosteroids comprised (n = 40, 32%) of total intraocular/periocular injections, with triamcinolone acetonide 10 or 40 mg (n = 19, 47.5%) most commonly used. 23 surgeons (58%) who utilized intraocular/periocular corticosteroids also prescribed topical corticosteroids. Topical nonsteroidal anti-inflammatory drugs were prescribed postoperatively by 148 surgeons (73%).Conclusions:Most surgeons prescribed topical AIM after routine cataract surgery. Many surgeons injected intraocular or periocular AIM while prescribing topical AIM. The diversity of practice patterns may reflect the lack of clear evidence-based guidelines.

100 Deals associated with MDCO-216

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Acute Coronary Syndrome	Phase 2	-	The Medicines Company (Spain) SL	-
Acute Coronary Syndrome	Phase 2	-	Esperion Therapeutics, Inc.	-
Acute Coronary Syndrome	Phase 2	-	Pfizer Inc.	-
Acute Coronary Syndrome	Phase 2	HU	The Medicines Co.	-
Acute Coronary Syndrome	Phase 2	CZ	The Medicines Co.	-
Acute Coronary Syndrome	Phase 2	CA	The Medicines Co.	-
Acute Coronary Syndrome	Phase 2	NL	The Medicines Co.	-
Acute Coronary Syndrome	Phase 2	US	The Medicines Co.	-
Acute Coronary Syndrome	Phase 2	PL	The Medicines Co.	-
Coronary Artery Disease	Phase 2	-	The Medicines Company (Spain) SL	-

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02678923 (MILANO-PILOT, Pubmed \| JAMA Cardiol) Manual	Phase 1/2	Acute Coronary Syndrome \| Coronary Disease	122	MDCO-216	(jdbveowgqz) = anitwldrbs jcrduwuodc (oeewubvnwc ) View more	Negative	01 Sep 2018
				Placebo	(jdbveowgqz) = xlaaeafntv jcrduwuodc (oeewubvnwc ) View more
NCT02678923 (PILOT \| MILANO-PILOT, CTgov)	Phase 1/2	Acute Coronary Syndrome \| Atherosclerosis	126	MDCO-216 (MDCO-216)	djmolgbnsk(ptzvbfkfkh) = coqvwreeju rbmdxlmrgt (wxjdwkycrq, uzrgelhfrr - kvbgfiuubl) View more	-	13 Jul 2017
				Placebo (Placebo)	djmolgbnsk(ptzvbfkfkh) = vseenuevel rbmdxlmrgt (wxjdwkycrq, ptszzvcija - lusyjbngdk) View more