Delving into the Latest Updates on Macozinone with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

MCZ

+ [2]

Target

DprE1

Action

inhibitors

Mechanism

DprE1 inhibitors(FAD-dependent decaprenylphosphoryl-beta-D-ribofuranose 2-oxidase inhibitors)

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication

Pulmonary TuberculosisTuberculosis

Inactive Indication-

Originator Organization

École Polytechnique Fédérale de Lausanne

Active Organization

Chemical Diversity Research Institute CJSCNearmedic Pharma Ltd.

École Polytechnique Fédérale de Lausanne

Inactive Organization

Nearmedic Plus Ltd.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC20H23F3N4O3S

InChIKeyBJDZBXGJNBMCAV-UHFFFAOYSA-N

CAS Registry1377239-83-2

This is a randomized, double-blind, placebo-controlled, multiple ascending dose study conducted at one study center in Switzerland.
Four (4) panels (A, B, C and D) of 8 male subjects (6 active and 2 placebo) each receiving multiple doses of PBTZ169 or a matching placebo, at increasing dose levels, once or twice daily.
Subjects will participate in only one panel. Blocks of 4 subjects (3 under active treatment, 1 under placebo) will be investigated in parallel. Panels will start sequentially.
Safety will be assessed throughout the study; serial ECGs and serial blood samples will be collected for the safety and PK assessment of PBTZ169.
Dose escalation will be allowed once the Trial Safety Board has determined that adequate safety and tolerability after each panel completion has been demonstrated to permit proceeding to the next panel.
In addition, a preliminary assessment of the drug interaction potential of PBTZ169 will be done by the measurement of inhibition or induction of human cytochromes through the metabolism of microdoses of standard probe substrates

Start Date21 Feb 2019

Sponsor / Collaborator

Pioneering Medicines

[+1]

NCT04150224

/ CompletedPhase 1

An Open-label, Prospective Study of Safety, Tolerability, Pharmacokinetics and Food Effects of PBTZ169, 80 mg Capsules, When Used in Ascending Doses in Healthy Volunteers

Open-label prospective non-comparative ascending dose randomized cohort study of single and multiple oral administration of PBTZ169 (capsules 80 mg) in healthy volunteers

Start Date03 Jul 2018

Sponsor / Collaborator

Nearmedic Plus Ltd.

NCT03423030

/ CompletedPhase 1

Safety, Tolerability, Pharmacokinetic Profile and Ex-vivo Antitubercular Activity of PBTZ169 Formulated as Spray- Dried Dispersion Versus Native Crystal Powder: Single Ascending Doses, Randomized, Placebo- Controlled, Cross-over Phase Ia Trial in Healthy Volunteers

This is a randomized, double-blind, placebo-controlled, single ascending dose study conducted at one study center in Switzerland.
Four (4) panels (A, B, C and D) of 8 male subjects (6 active and 2 placebo) each undergoing 2 investigation periods and receiving either single doses of PBTZ169 at increasing dose levels or a matching placebo.
Subjects will participate in only one panel. Blocks of 4 subjects (3 under active treatment, 1 under placebo) will be investigated in parallel. Panels A and B are interleaved.
Safety will be assessed throughout the study; serial ECGs and serial blood samples will be collected for the safety and PK assessment of PBTZ169.
Dose escalation will be allowed once the Trial Safety Board has determined that adequate safety and tolerability after panel B and panel C completion has been demonstrated to permit proceeding to the next panel.

Start Date05 Dec 2017

Sponsor / Collaborator

Pioneering Medicines

[+1]

100 Clinical Results associated with Macozinone

Login to view more data

100 Translational Medicine associated with Macozinone

Login to view more data

100 Patents (Medical) associated with Macozinone

Login to view more data

211

Literatures (Medical) associated with Macozinone

01 May 2025·Talanta

Exploring wood-derived biochar potential for electrochemical sensing of fungicides mancozeb and maneb in environmental water samples

Article

Author: Anojčić, Jasmina ; Petrović, Jelena ; Apostolović, Tamara ; Mutić, Sanja ; Beljin, Jelena ; Đukanović, Nina ; Simetić, Tajana

The sustainable material, biochar (BC) from a hardwood source, was synthesized via pyrolysis process at 400 °C (BC400) and 700 °C (BC700) and used as a modifier during the electrochemical sensor design. The prepared BCs were characterized by scanning electron microscopy (SEM), Brunauer-Emmett-Teller (BET) analysis, and elemental analysis (CHNS). The development of rapid analytical techniques for detecting pesticides employing a low-cost carbon paste electrode (CPE) modified with BC is a novel strategy to provide a sensitive response to water pollution. The prepared working electrodes (unmodified CPE, BC400-CPE, and BC700-CPE) were compared for selected fungicides mancozeb (MCZ) and maneb (MAN) sensing, and BC700-CPE provides the most favorable analytical response of target analytes. Cyclic voltammetric investigations revealed that the electrode reaction is irreversible and controlled by the adsorption of MCZ and MAN at the surface of the BC700-CPE, which led to an optimization of the differential pulse adsorptive stripping voltammetric (DP-AdSV) method. The obtained working linear concentration ranges were 25-2780 μg L^-1 MCZ and 49-1840 μg L^-1 MAN in Britton-Robinson buffer pH 7.0 using CPE modified with 10 % BC700. The evaluated limit of detection was 7.5 μg L^-1 for MCZ and 15.0 μg L^-1 for MAN. Investigated interferences did not significantly affect the MCZ and MAN oxidation signal intensity. The developed DP-AdSV method was successfully applied to determine selected fungicides in spiked river water and wastewater samples, with good recovery and reproducibility.

01 Apr 2025·European Journal of Pharmacology

Biochemical insights into synergistic Candida biofilm disintegrating ability of p-cymene inclusion complex and miconazole

Article

Author: Yadav, Bhawana ; Poluri, Krishna Mohan ; Kumar, Amit ; Mishra, Purusottam ; Roy, Ankita ; Gupta, Payal

Phytoactive molecules emerge as a plentiful reservoir of adjuvant and antifungal agents. The resolution of solubility and stability issues has been facilitated by developing molecular complexes or inclusion complexes of phytoactive molecules. Miconazole (MCZ) is a favoured azole with low off-target impact, however, its pharmacological efficacy requires a revamp to enhance its suitability as an antifungal drug. Hence, the present investigation delves into the mechanism of action of the p-cymene/β-cyclodextrin inclusion complex (IC) along with MCZ against Candida albicans and Candidaglabrata biofilms. The synergy between IC and MCZ has been estimated at a concentration of 6.25 μg/mL IC + 0.5 μg/mL MCZ with a FICI of 0.19. The prepared IC + MCZ displayed remarkable antifungal properties against planktonic and sessile growth of Candida species. IC + MCZ exhibited a notable 80% biofilm eradication potential against both species, corroborated by morphological analysis using FE-SEM. The results indicated that IC/IC + MCZ acts by disrupting the biochemical composition of the ECM, altering the surface properties of the cells, reducing ergosterol, enhancing membrane permeability, and inducing oxidative stress. In conclusion, the study highlighted the synergistic antibiofilm activity of p-cymene IC with miconazole against Candida species. In summary, IC + MCZ has been established as a potent antifouling agent against Candida species, warranting further exploration for potential formulation with additional investigations.

01 Apr 2025·Chemosphere

Mancozeb exposure disrupts endocrine function of the ovary and thyroid in Red Munia (Amandava amandava)

Article

Author: Mohanty, Banalata

Mancozeb (MCZ), a dithiocarbamate fungicide, has the potential to disrupt thyroid hormone (TH) functioning in non-target organisms. THs play a crucial role in seasonal reproduction and previous studies have shown that even low levels of MCZ exposure can affect thyroid and testicular function in the Red Munia bird (Amandava amandava), a distinct seasonal breeder. This study specifically examines the impact of MCZ exposure on female Red Munia to investigate any sex-specific effects. Exposure to sublethal levels (0.5% LD50) of MCZ for 30 consecutive days during the critical transition to the breeding phase disrupts the pituitary-ovarian and pituitary-thyroid axes in Red Munia. The morphometry (number/size/immunointensity) of pituitary luteinizing hormone (LH) and thyroid-stimulating hormone (TSH) producing cells, immunoreacted with anti-human (h) LHβ/anti-chicken (c) LHβ, and anti-hTSH β respectively, was significantly altered. Plasma levels of LH (p < 0.01), follicle-stimulating hormone (p < 0.001), and TSH (p < 0.01) were significantly decreased. There was a significant increase in the number of atretic primordial and primary follicles, thinning and disorganization of the granulosa cell layers in maturing follicles, and significant decrease in plasma levels of estradiol (p < 0.001).The reduced diameter of the thyroid gland, a significant increase in empty follicles, and a decrease in plasma levels of THs (T3, p < 0.01; T4, p < 0.001), indicate disruption of thyroid function. It is not only MCZ and its residual products, but also the inert ingredients in the commercial formulation/metabolites, may have contributed to the interference with thyroid function during the transition to the breeding phase to compromise ovarian recrudescence in the Red Munia bird.

100 Deals associated with Macozinone

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14821

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Pulmonary Tuberculosis	Phase 2	-	École Polytechnique Fédérale de Lausanne	-
Tuberculosis	Preclinical	Russia	Chemical Diversity Research Institute CJSC	14 Nov 2022
Tuberculosis	Preclinical	Russia	Nearmedic Pharma Ltd.	14 Nov 2022

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03036163 (CTgov)	Phase 1	Tuberculosis	40	PBTZ169 - 40 mg (Cohort 1)	ynxgevydzw(jwwbvyuknz) = vzwnzkkmyz izgyenpcvu (lsiwzdmgfv, ohjvtrjuey - yupvpopllk) View more	-	13 Apr 2020
				PBTZ169 - 80 mg (Cohort 2)	ynxgevydzw(jwwbvyuknz) = esantdmzhr izgyenpcvu (lsiwzdmgfv, wrpqxxtcgz - mdkgylblvg) View more
NCT03334734 (CTgov)	Phase 2	Pulmonary Tuberculosis	16	PBTZ169 (PBTZ169, 160 mg)	(auwmukhowh) = shbgzvvslj ltawpgzyyw (odvxyhjgqz, arwtanpnap - lbphueofcj) View more	-	09 Mar 2020
				PBTZ169 (PBTZ169, 320 mg)	(auwmukhowh) = vunugcqkrn ltawpgzyyw (odvxyhjgqz, higyjdxpaa - ydfdkkxspk) View more
NCT04150224 (CTgov)	Phase 1	-	60	PBTZ169 960 mg SD (Cohort 2 (C2), PBTZ169)	wvvaptwdcj(havgetyxlm) = zgfsvioulf ckvbdsukwj (fmvfvptsks, gzmvbtqfzv - aoziiszpmh) View more	-	28 Feb 2020
				PBTZ169 640 mg BiD (Cohort 3 (C3), PBTZ169)	wvvaptwdcj(havgetyxlm) = ktiuwqtgcw ckvbdsukwj (fmvfvptsks, xjssvwjlkx - bdjliphxya) View more