A Two Arm, Randomized, Multicenter, Single blind, Prospective, Clinical study to evaluate efficacy & safety of PS/MAR/HO-1 oil and a marketed formulation in mild to moderate Hair loss in females - NIL

开始日期2015-05-16

申办/合作机构

Marico Ltd.

100 项与 HO-1(Metabomed) 相关的临床结果

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100 项与 HO-1(Metabomed) 相关的转化医学

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100 项与 HO-1(Metabomed) 相关的专利（医药）

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209

项与 HO-1(Metabomed) 相关的文献（医药）

2024-12-31·Journal of enzyme inhibition and medicinal chemistry

Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells

Article

作者: Salerno, Loredana ; Giuliano, Michela ; Notaro, Antonietta ; Intagliata, Sebastiano ; Affranchi, Federica ; Consoli, Valeria ; Sorrenti, Valeria ; Pittalà, Valeria ; Vanella, Luca

Colon cancer remains a clinical challenge in industrialised countries. Its treatment with 5-Flurouracil (5-FU) develops many side effects and resistance. Thus, several strategies have been undertaken so far, including the use of drug cocktails and polypharmacology. Heme oxygenase-1 (HO-1) is an emerging molecular target in the treatment of various cancers. We recently demonstrated that a combination of HO-1 inhibitors with 5-FU and the corresponding hybrids SI1/17, SI1/20, and SI1/22, possessed anticancer activity against prostate and lung cancer cells. In this work, we evaluated these hybrids in a model of colon cancer and found that SI1/22 and the respective combo have greater potency than 5-FU. Particularly, compounds inhibit HO-1 activity in cell lysates, increase ROS and the expression of HO-1, SOD, and Nrf2. Moreover, we observed a decrease of pro-caspase and an increase in cleaved PARP-1 and p62, suggesting apoptotic and autophagic cell death and potential application of these drugs as anticancer agents.

2024-09-12·ACS Medicinal Chemistry Letters

Highly Selective Novel Heme Oxygenase-1 Hits Found by DNA-Encoded Library Machine Learning beyond the DEL Chemical Space

Article

作者: Hsueh, Kuang-Lung ; Deng, Jason ; Song, Yidan ; He, Yunyun ; Han, Shuai ; Su, Wenji ; Guo, Xinyun ; Wang, Min ; Kuai, Letian ; Liu, Huan ; Cui, Weiren

DNA-encoded library (DEL) technology, especially when combined with machine learning (ML), is a powerful method to discover novel inhibitors. DEL-ML can expand a larger chemical space and boost cost-effectiveness during hit finding. Heme oxygenase-1 (HO-1), a heme-degrading enzyme, is linked to diseases such as cancer and neurodegenerative disorders. The discovery of five series of new scaffold HO-1 hits is reported here, using a DEL-ML workflow, which emphasizes the model's uncertainty quantification and domain of applicability. This model exhibits a strong extrapolation ability, identifying new structures beyond the DEL chemical space. About 37% of predicted molecules showed a binding affinity of K _D < 20 μM, with the strongest being 141 nM, amd 14 of those molecules displayed >100-fold selectivity for HO-1 over heme oxygenase-2 (HO-2). These molecules also showed structural novelty compared to existing HO-1 inhibitors. Docking simulations provided insights into possible selectivity rationale.

2024-05-01·Pancreatology : official journal of the International Association of Pancreatology (IAP) ... [et al.]

Intravenous Hemin, a potential heme oxygenase-1 activator, does not protect from post-ERCP acute pancreatitis in humans: Results of a randomized multicentric multinational placebo-controlled trial

Article

作者: Verset, Didier ; Njimi, Hassane ; Hittelet, Axel ; Devière, Jacques ; Margos, Walter ; Le Moine, Olivier ; Arvanitakis, Marianna ; Yared, Rawad A ; Liao, Wei-Chih ; Delhaye, Myriam ; Huberty, Vincent ; Toussaint, Emmanuel ; Viesca, Michael Fernandez Y ; Lemmers, Arnaud ; Chen, Chieh-Chang ; Vandorpe, Astrid ; Blero, Daniel

OBJECTIVE:

Hemin, a heme oxygenase 1 activator has shown efficacy in the prevention and treatment of acute pancreatitis in mouse models. We conducted a randomized controlled trial (RCT) to assess the protective effect of Hemin administration to prevent post-endoscopic retrograde cholangiopancreatography (ERCP) pancreatitis (PEP) in patients at risk.

METHODS:

In this multicenter, multinational, placebo-controlled, double-blind RCT, we assigned patients at risk for PEP to receive a single intravenous dose of Hemin (4 mg/kg) or placebo immediately after ERCP. Patients were considered to be at risk on the basis of validated patient- and/or procedure-related risk factors. Neither rectal NSAIDs nor pancreatic stent insertion were allowed in randomized patients. The primary outcome was the incidence of PEP. Secondary outcomes included lipase elevation, mortality, safety, and length of stay.

RESULTS:

A total of 282 of the 294 randomized patients had complete follow-up. Groups were similar in terms of clinical, laboratory, and technical risk factors for PEP. PEP occurred in 16 of 142 patients (11.3%) in the Hemin group and in 20 of 140 patients (14.3%) in the placebo group (p = 0.48). Incidence of severe PEP reached 0.7% and 4.3% in the Hemin and placebo groups, respectively (p = 0.07). Significant lipase elevation after ERCP did not differ between groups. Length of hospital stay, mortality and severe adverse events rates were similar between groups.

CONCLUSION:

We failed to detect large improvements in PEP rate among participants at risk for PEP who received IV hemin immediately after the procedure compared to placebo.

TRIAL REGISTRATION NUMBER:

ClinicalTrials.gov number, NCT01855841).

100 项与 HO-1(Metabomed) 相关的药物交易

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