Delving into the Latest Updates on Ombitasvir with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ombitasvir, Ombitasvir (USAN), ABT-267

Target

NS5A

Action

inhibitors

Mechanism

NS5A inhibitors(Nonstructural protein 5A inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System Disorders

Active Indication-

Inactive Indication

Chronic hepatitis C genotype 1Chronic hepatitis C genotype 1bChronic hepatitis C genotype 3

Originator Organization

AbbVie, Inc.

Active Organization-

Inactive Organization

AbbVie, Inc.

Abbott Laboratories

License Organization-

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC50H67N7O8

InChIKeyPIDFDZJZLOTZTM-KHVQSSSXSA-N

CAS Registry1258226-87-7

This prospective, multi-center, observational study is designed to assess the real world effectiveness of paritaprevir/r - ombitasvir with dasabuvir (3DAA [direct-acting antiviral agent] ABBVIE REGIMEN) without ribavirin (RBV) and to describe baseline characteristics of participants with chronic hepatitis C virus (HCV) genotype 1b (GT1b) infection and compensated liver cirrhosis in Russia.

Start Date20 Mar 2017

Sponsor / Collaborator

AbbVie, Inc.

NCT03002818

/ CompletedNot Applicable

Quality of Life Measurement Using Wrist Actigraphy in HCV Genotype 1 Infected, Treatment naïve Patients Suffering From Fatigue and Receiving Ombitasvir, Paritaprevir, and Ritonavir Tablets and Dasabuvir Tablets (Viekirax®/Exviera®; 3D Regimen): The HEMATITE Study

This is an observational, prospective, open-label, single-arm, multicenter, real-life study designed to observe the impact of paritaprevir/ritonavir/ombitasvir with dasabuvir regimen (Viekirax®/Exviera®, 3D regimen) on total daytime physical activity and fatigue in participants with HCV GT1.

Start Date01 Mar 2017

Sponsor / Collaborator

AbbVie, Inc.

JPRN-UMIN000026640

/ CompletedNot ApplicableIIT

Predictive factors associated with virological response in Ombitasvir/Paritaprevir/Ritonavir/Ribavirin combination therapy for genotype2a infected chronic hepatitis C patients - Virological response in Ombitasvir/Paritaprevir/Ritonavir/Ribavirin combination therapy for genotype2a infected chronic hepatitis C patients

Start Date16 Jan 2017

Sponsor / Collaborator-

100 Clinical Results associated with Ombitasvir

Login to view more data

100 Translational Medicine associated with Ombitasvir

Login to view more data

100 Patents (Medical) associated with Ombitasvir

Login to view more data

1,040

Literatures (Medical) associated with Ombitasvir

01 Aug 2025·JOURNAL OF PHARMACEUTICAL SCIENCES

Investigating the effect of permeation enhancers on oral absorption of a BCS IV compound, ombitasvir, utilizing animal models

Article

Author: Hanouch, Layan ; Borchardt, Thomas ; Gignac, Nathan ; Marsh, Kennan ; Indulkar, Anura S

Discovery of complex biological targets and novel treatment modalities have led to an increase in the number of compounds with poor permeability. Generally, formulation design and development are primarily focused on overcoming poor solubility. Improving oral bioavailability by utilizing permeation enhancers for poorly permeable new chemical entities (NCEs) has not been widely explored. Therefore, in this work the effect of permeation enhancers on a poorly soluble and poorly permeable compound, ombitasvir (OBT), was investigated. Structurally diverse permeation enhancers (PEs) with good safety profile-labrasol® ALF, lauroyl L- and palmitoyl L-carnitine, salcaprozoate sodium (SNAC), and sodium caprate-were tested. To study the impact of solid form and formulation, OBT was dosed as crystal form and as amorphous formulations. To avoid the influence of preclinical in vitro/ex vivo method artifacts on data interpretation, studies were conducted in whole animal models (rat and dog). OBT was dosed at 2 mg/kg and PEs were dosed at 20 mg/kg by peroral route. In rats, OBT was administered as an amorphous colloidal suspension. Only the carnitines showed meaningful enhancement (∼2X) in oral bioavailability. In dogs, OBT was dosed in enteric capsules as crystal form, a slow dissolving 15 % drug load (DL) amorphous solid dispersion (ASD) that slowly reached amorphous solubility, and a rapidly dissolving 5 % DL ASD that reached amorphous solubility and formed amorphous nanoprecipitates, with and without PEs. OBT was not detected in the blood upon dosing of neat crystalline solid. However, when co-dosed with PEs significantly high oral bioavailability (11-17 %) was observed. 15 % DL ASD alone showed a meaningful increase in oral bioavailability (∼4 %) relative to the crystal form; and combination with PEs further increased the bioavailability by 2-5 fold. All the PEs showed enhancement in oral bioavailability when combined with the crystal form and 15 % DL ASD. The enhancement in bioavailability due to SNAC was attributed to dissolution rate enhancement whereas, that due to lauroyl L-carnitine and labrasol was attributed to both dissolution and permeability enhancement. 5 % DL ASD by itself increased the oral bioavailability to ∼8 % which was attributed to its rapid dissolution. A massive increase in the oral bioavailability to 78 % (∼10-fold enhancement) was observed with lauroyl L-carnitine. In contrast to the crystal form and 15 % DL ASD groups, other PEs, were found to be ineffective when combined with the 5 % DL ASD. Physicochemical characterization including solubility determination in presence of PEs, dissolution performance of the forms/formulations and particle size distribution of the amorphous precipitated phase (for 5 % DL ASD) in presence of PEs was performed to understand in vivo results. It was concluded that the dissolution rate of the form/formulation, the amount of drug concomitantly available with PE at the site of absorption, the association of PE with the precipitated amorphous phase and the particle size of this phase impacts the overall performance of PE towards improving oral bioavailability. The results of this study present promising approaches to formulate BCS IV compounds.

13 Apr 2025·Cureus Journal of Medical Science

The Impact of Organic Anion-Transporting Polypeptide (OATP) Variants on the Side Effects of Direct-Acting Antivirals in Hepatitis C Patients

Article

Author: Altintas, Zuhal ; Altintas, Engin

Background Organic anion-transporting polypeptides (OATPs) are responsible for the cellular uptake of a broad range of endogenous compounds and xenobiotics in multiple tissues. The aim of our study was to determine whether variations in OATP1B1 and OATP1B3 affect the side effects experienced by hepatitis C patients treated with direct-acting antivirals (DAAs). Methods This study included 199 hepatitis C patients treated with DAAs. Ledipasvir/sofosbuvir or ombitasvir/paritaprevir/ritonavir ± dasabuvir and 162 control individuals without hepatitis C. Treatment-related side effects were recorded. The OATP1B1 gene variations c.388A>G and c.521T>C and the OATP1B3 gene variations c.334T>G and c.699G>A were analyzed via the polymerase chain reaction-restriction fragment length polymorphism method. Allele/genotype combinations of OATP1B1 and OATP1B3 haplotypes were evaluated. Results Side effects were observed in 53 (26.6%) of 199 hepatitis C patients. There were skin mucosal lesions in 19 patients (36%), fatigue in 18 patients (34%), pruritus in 11 patients (20.5%), and other in five patients (9.5%). There was a significant relationship between the c.334T>G variant and side effects (p = 0.030). The frequency distribution of the c.334T>G variant was in Hardy-Weinberg equilibrium. The frequencies of the patient group and the control group were 65.3% and 63%, respectively. We found a significant difference between the patient and control groups in terms of the haplotype ratios of c.388A>G and c.521T>C (p = 0.036). Conclusions We found a significant relationship between the c.334T>G variant in OATP1B3 and DAA-related side effects in hepatitis C patients.

01 Feb 2025·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Pyrrolidine SS13 induces oxidative stress and autophagy-mediated cell death in colorectal cancer cells

Article

Author: Keselakova, Alexandra ; Majirska, Monika ; Pilatova, Martina Bago ; Martinkova, Miroslava ; Kello, Martin ; Mirossay, Andrej ; Nosalova, Natalia ; Fabianova, Dominika

INTRODUCTION:

Pyrrolidines, nitrogenous organic compounds, are among the most intensively studied agents because of their antibacterial, antiviral, neurological, and promising antitumor effects. Moreover, many medicinal drugs contain pyrrolidine moiety such as sunitinib (anticancer drug), telaprevir and ombitasvir (antiviral drugs) or ramipril (antihypertensive drug).

RATIONALE OF THE STUDY:

Based on the pro-apoptotic effect of pyrrolidine SS13, this study focuses on the pro-oxidative properties of the tested pyrrolidine SS13 on colorectal cancer cells to deepen the understanding of its mechanisms of action.

RESEARCH HYPOTHESIS:

We hypothesize that SS13 induces oxidative stress and autophagy activation in HCT116 and Caco-2 cell lines, thus contributing to antiproliferative effects.

METHODS:

Flow cytometry, western blot, fluorescence microscopy and qRT-PCR were used to evaluate the effect of pyrrolidine SS13.

CONCLUSION AND FUTURE DIRECTIONS:

Pyrrolidine SS13 induced oxidative stress through the accumulation of reactive oxygen and nitrogen species in both cell lines and the modulation of both superoxide dismutase isoenzymes (SOD1, SOD2). Oxidative stress was also associated with the activation of DNA damage response system and modulation of stress/survival pathways. We demonstrated for the first time that pyrrolidine SS13 is involved in the induction of autophagy accompanied by increased levels of autophagic markers (p-AMPK, p-ULK, LC3I/II and ATG7) and a significant decrease in p62 protein levels in both cell lines. Finally, chloroquine, an inhibitor of autophagy, enhanced cell survival and suppressed the cytotoxic effect of SS13 in HCT116 and Caco-2 cells, indicating that SS13 contributes to autophagy-mediated cell death. Taken together, our results suggest that oxidative stress and autophagy participate in the antiproliferative effect of pyrrolidine SS13 on colorectal cancer cells. Further research using primary cell cultures obtained from different animal tissues as well as performing in vivo experiments is needed to understand these processes in detail and to investigate the potential therapeutic application of new pyrrolidine derivatives.

1

News (Medical) associated with Ombitasvir

12 Dec 2023

·synapse.patsnap.com

What are NS5A inhibitors and how do you quickly get the latest development progress?

NS5A is a crucial protein found in the human body that plays a significant role in the life cycle of the hepatitis C virus (HCV). It is involved in viral replication, assembly, and release, making it an attractive target for antiviral therapies. NS5A interacts with various host proteins and cellular pathways, modulating the immune response and promoting viral persistence. Inhibiting NS5A can disrupt HCV replication, leading to reduced viral load and improved clinical outcomes. Understanding the function of NS5A is essential for developing effective treatments against HCV and combating the global burden of this infectious disease. The analysis of the current competitive landscape of target NS5A reveals that Gilead Sciences, Inc., AbbVie, Inc., and Merck & Co., Inc. are the leading companies in terms of R&D progress. These companies have drugs in multiple phases of development, including the approved phase. The indication analysis shows that drugs under the target NS5A have been approved for various indications related to Hepatitis C, Fibrosis, Cirrhosis, and other diseases. The drug types progressing most rapidly are small molecule drugs and synthetic peptides, indicating intense competition in the market. China is a significant player in the development of drugs targeting NS5A, with the highest number of drugs in the approved phase. Other countries such as Japan, European Union, and the United States also have a considerable presence in the development of NS5A drugs. The future development of target NS5A is promising, with ongoing research and development by various companies and institutions. The competition in the market is expected to intensify, especially for small molecule drugs and synthetic peptides. Further advancements in the treatment of Hepatitis C and other related indications can be expected with the continued efforts of the pharmaceutical industry. How do they work?NS5A inhibitors are a type of antiviral medication that target the NS5A protein in the hepatitis C virus (HCV). From a biomedical perspective, these inhibitors work by blocking the function of the NS5A protein, which is essential for viral replication and assembly. By inhibiting NS5A, these drugs help to prevent the spread and multiplication of the hepatitis C virus in the body. NS5A inhibitors are commonly used in combination with other direct-acting antiviral drugs to treat chronic hepatitis C infection. They have shown high efficacy in achieving sustained virologic response (SVR), which means that the virus is undetectable in the blood six months after completing treatment. These inhibitors have revolutionized the treatment of hepatitis C, offering shorter treatment durations, improved tolerability, and higher cure rates compared to older therapies. It's important to note that NS5A inhibitors are specific to the treatment of hepatitis C and are not used for other viral infections or diseases. They are typically prescribed by healthcare professionals and should be taken as directed to ensure optimal treatment outcomes. Common examples of NS5A inhibitors include ledipasvir, daclatasvir, and ombitasvir. List of NS5A InhibitorsThe currently marketed NS5A inhibitors include: Emitasvir PhosphateRavidasvir HydrochlorideCoblopasvir hydrochlorideGlecaprevir/PibrentasvirGlecaprevir/PibrentasvirElbasvirSofosbuvir/VelpatasvirElbasvir/GrazoprevirOmbitasvir/Paritaprevir/RitonavirLedipasvir/SofosbuvirFor more information, please click on the image below. What are NS5A inhibitors used for?NS5A inhibitors are commonly used in combination with other direct-acting antiviral drugs to treat chronic hepatitis C infection. For more information, please click on the image below to log in and search. How to obtain the latest development progress of NS5A inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of NS5A inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Ombitasvir

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D10576	Ombitasvir	-	DB09296

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Chronic hepatitis C genotype 1b	Phase 2	-	AbbVie, Inc.	01 Aug 2012
Chronic hepatitis C genotype 3	Phase 2	-	AbbVie, Inc.	01 Sep 2011
Chronic hepatitis C genotype 1	Phase 2	United States	AbbVie, Inc.	01 Mar 2011
Chronic hepatitis C genotype 1	Phase 2	Puerto Rico	AbbVie, Inc.	01 Mar 2011

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02486406 (ZIRCON, Pubmed \| Adv Ther) Manual	Phase 2/3	Hepatitis C	26	OBV+ PTV+ritonavir+ DSV+DSV+ribavirin	dyoaxctifh(qpyfjzwxsg) = xtdutatelz xjilsvuipg (ifzpozgfuz, 81.1 - 99.3) View more	Positive	01 Jul 2020
P1384 (ERA2020)	Not Applicable	Renal Insufficiency \| Hepatitis C, Chronic hemoglobin \| serum creatinine	235	Direct Acting Anti-Virus (Anemic CKD patients)	xkqhfhiceq(cyabysuzhs) = jzbbshzqlt rrniryfqxi (hhdpqqiedi ) View more	Positive	06 Jun 2020
P1384 (ERA2020)	Not Applicable		235	Direct Acting Anti-Virus (Non-anemic CKD patients)	xkqhfhiceq(cyabysuzhs) = lsukewufnh rrniryfqxi (hhdpqqiedi ) View more	Positive	06 Jun 2020
SP138 (ERA2019)	Not Applicable	Kidney Failure, Chronic \| Hepatitis C, Chronic	53	Ombitasvir 50 mg / Paritaprevir 150 mg / Ritonavir 100 mg	bqexxmblwr(nhbrafuied) = Anemia was observed during in 7 patients (13.2%), which required transfusion, erythropoietin therapy, and modification of RBV dose to be every other day giplytqodh (diorooffvv )	Positive	13 Jun 2019
EASL2019	Not Applicable	Fibrosis, Liver \| Hepatitis C	3,067	Ombitasvir/Paritaprevir/Ritonavir and Dasabuvir 8 weeks	vfnjvxgxeh(feipcdegad) = jiiaewzjir mfbokckkgh (pblfmyiejk )	Positive	11 Apr 2019
EASL2019	Not Applicable	Fibrosis, Liver \| Hepatitis C	3,067	Ombitasvir/Paritaprevir/Ritonavir and Dasabuvir 12 weeks	vfnjvxgxeh(feipcdegad) = woqeuadywl mfbokckkgh (pblfmyiejk )	Positive	11 Apr 2019
NCT01609933 (Pubmed)	Phase 2	Chronic hepatitis C genotype 1	32	Ombitasvir, paritaprevir, and ritonavir	aqevpligim(yyesahotzu) = irrdaisjae mrmynhwqdp (zeumnytkes )	Positive	01 Jan 2019
UEGW2018	Not Applicable	Liver Cirrhosis increased total bilirubin \| prolonged INR	5,853	Ombitasvir, Paritaprevir/ r+Dasabuvir+Ribavirin	lbsszjircm(jkrutfkgsc) = 4 thxfkioimr (bedhtkflll ) View more	Positive	01 Oct 2018
UEGW2018	Not Applicable	HCV	22	DAA- resection+ RFA	lwusnycado(jbivrktphd) = Two female patients died of acute liver insufficiency (9.5%) one after completing 12 weeks of treatment, and the other in week 7 of DAA therapy (in the DAA- resection+ RFA group) sveqcogggb (qflmahdrby ) View more	Positive	01 Oct 2018
UEGW2018	Not Applicable	HCV	22	Control- resection+ RFA		Positive	01 Oct 2018
UEGW2016	Not Applicable	Compensated cirrhosis	-	Ombitasvir / Paritaprevir / Ritonavir + Dasabuvir + Ribavirin	uytswymkah(kkkyllccqp) = 2% wniicmdpnz (voqlolhwri ) View more	-	01 Oct 2016
NCT01458535 (Navigator, CTgov)	Phase 2	Chronic hepatitis C genotype 3	61	ABT-450+ribavirin+ritonavir+ABT-267 (ABT-450/r and ABT-267 Plus RBV in Genotype 1 Participants)	sjteeahouf = oglbewzumq vnadnyhxjh (obfytmodma, kzzqskxdvj - zwruyzafaj) View more	-	11 Jul 2016
NCT01458535 (Navigator, CTgov)	Phase 2	Chronic hepatitis C genotype 3	61	ABT-450+ribavirin+ritonavir+ABT-267 (ABT-450/r and ABT-267 Plus RBV in Genotype 2 Participants)	sjteeahouf = gtcvnloaib vnadnyhxjh (obfytmodma, ehpvstgxbn - wmwujmnduq) View more	-	11 Jul 2016
PEARL-II \| PEARL-III \| TURQUOISE-II (UEGW2015)	Phase 3	Chronic hepatitis C genotype 1b IL28B non-CC genotype \| baseline viral loads â¥800,000 IU/mL	369	Ombitasvir/Paritaprevir/Ritonavir and Dasabuvir	zoklhzeidz(lwlrmgepgm) = 0.3% somoldyiat (jyelaqoslf ) View more	Positive	01 Oct 2015