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estradiol (E2III)

✓ Approved

Johnson & Johnson Services, Inc. · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Johnson & Johnson Services, Inc.. It is approved for therapeutic indications via transdermal.

Drug Profile

Brand NamesE2III
CompanyJohnson & Johnson Services, Inc.
Drug ClassSmall Molecule
Molecular TargetESR1
RouteTransdermal
StatusApproved
Sources: ClinicalTrials.gov, Johnson & Johnson Services, Inc.

Mechanism of Action

Molecular Targets

estradiol acts on 1 molecular target:

ESR1estrogen receptor 1 (ER, ESR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

estradiol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Surgical and medical proceduresHormone replacement therapy✓ Approved

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PubMedChemistry (Weinheim an der Bergstrasse, Germany)2026-10-15

A Green Protocol for the Deprotection of ortho-Nitrobenzyl Esters and Ethers by UVA-LED Irradiation.

Poikilidou Despoina D, Mantzourani Christiana C, Kokotos George G, Kokotos Christoforos G CG

The removal of protecting groups in synthetic organic transformations under green and mild conditions is of high interest. In this study, a green photochemical protocol for the deprotection of ortho-nitrobenzyl esters and ethers is introduced, utilizing LED 370 nm irradiation and methanol as the solvent in a short reaction time. This method was demonstrated in a number of substrates and applied in the synthesis of a cytosolic phospholipase A2 inhibitor. Direct infusion-high resolution mass spectrometry contributed to the study of the photo-release mechanism.

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PubMedFrontiers in pharmacology2026-10-15

Mapping the antileishmanial structure-activity relationship of eugenol.

Daut Lucas L, Taylor Jonathan J, Carter Nicola S NS, Stamper Brendan D BD

Leishmaniasis is a neglected tropical disease with a devastating global impact. The current medications on the market for treating this protozoan parasitic infection are insufficient to fit the global need, with long durations of therapy, growing resistance rates, and severe adverse effects. This investigation aims to characterize an antileishmanial structure-activity relationship for the natural product eugenol. With Leishmania donovani as a model, a series of dose-response curves were performed against eugenol and several of its structural analogs. The same set of compounds was tested against the human monocyte cell THP-1 to characterize their selective toxicity. Subsequently, the pharmacokinetic parameters of the tested compounds were estimated using the in silico modelling software, Percepta®. Eugenol and its analogs demonstrated varying levels of antileishmanial potency, with 4-allylphenol (chavicol) as the most potent compound tested and with the most promising selectivity index. In comparing the potencies and structures of the compounds tested, the data suggests that the para-substituted allyl tail and the phenolic group are important to conferring potency, while the ortho-methoxy substitutions decreased potency. Furthermore, the pharmacokinetic properties of these compounds were predicted to closely resemble eugenol with little risk of cytochrome P450 (CYP) interactions. While more testing is needed to confirm the mechanisms and safety of these compounds, these results suggest eugenol analogs show promise as future antileishmanial therapies.

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Hair Steroid Signatures of Cooperative Breeding in Male and Female Common Marmosets (Callithrix jacchus).

Laubi Benjamin N BN, Glauser Gaëtan G, Willems Erik P EP, van Schaik Carel P CP et al.

Cooperative breeding presents social and reproductive challenges that differ from those associated with independent breeding, but its endocrine correlates are not well understood. We investigated cumulative steroid hormone profiles in common marmosets (Callithrix jacchus), a primate species characterized by shared caregiving and clearly defined reproductive roles between primary breeders and non-breeding helper group members. Using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) on hair samples, we simultaneously quantified six steroid hormones across 71 individuals varying in breeding role, sex, age, and group reproductive context. Glucocorticoids were highest in breeder females, declined with age, and were higher in breeders when dependent offspring were present. Testosterone showed a comparatively modest male-female difference and was positively associated with the presence of dependent offspring in breeders, whereas androstenedione closely paralleled testosterone across age, consistent with shared regulation. Ovarian steroids showed clear sex differentiation in progesterone, with markedly elevated levels in breeder females, whereas estradiol differences were smaller, emerging as a modest sex effect within breeders and an age effect in helpers. Together, these findings highlight weaker sexual dimorphism in sex hormone profiles than often reported for independently breeding primates. They also reveal hormonal signatures of stress and vigilance related to caregiving, consistent with cooperative breeding in marmosets. Our study demonstrates the value of hair for long-term hormonal assessment and underscores the utility of HPLC-MS/MS for quantifying multiple hormones with high specificity in socially complex primates. The online version contains supplementary material available at https://doi.org/10.1007/s10764-026-00568-9.

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Rational structure-guided identification of a Bcl-2-targeting peptide with antiproliferative effects on colorectal cancer cells.

Jin Xing X, Yang Shudan S, Wang Qianqian Q, Chen Shutong S et al.

Bcl-2 is critical for tumour survival and serves as a promising anticancer drug target. Herein, a series of novel Bcl-2-targeted peptides were identified through structure-based virtual screening and systematic biological validation. Four candidate peptides were selected from the peptide library. MST results demonstrated that Peptide 1 exhibited the strongest apparent binding affinity towards Bcl-2 (Kd = 0.51 ± 0.03 μM), superior to VS-9 and other screened peptides. Molecular dynamics simulation, free energy landscape analysis, and MM/GBSA calculation further supported the predicted conformational features of the Bcl-2-Peptide-1 complex. MTT assays demonstrated that Peptide-1 markedly inhibited the proliferation of HT29 and Colo320HSR colorectal cancer cells, while showing limited effects on normal NCM460 cells. Bcl-2 knockdown attenuated the bioactivity of Peptide-1, and RT-qPCR and ELISA analyses revealed that Peptide-1 modulated Bax/Bcl-2 expression at both transcriptional and protein levels. Peptide-1 represents a promising Bcl-2-targeting peptide with antiproliferative activity against colorectal cancer cells.

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Which Injection Is More Effective for Partial-Thickness Rotator Cuff Tear? Atelocollagen Versus Acellular Dermal Matrix.

Lee Kyoung-Geun KG, Cho Sung-Hyun SH, Kim Yang-Soo YS

Collagen-inducing injections are emerging as new treatments for partial-thickness rotator cuff tears (PTRCTs). This study aimed to directly compare the effects of atelocollagen and acellular dermal matrix (ADM) injections on PTRCTs. Between July 2019 and December 2021, 183 patients with PTRCTs who were treated with ultrasound-guided collagen injections were retrospectively enrolled. Two injections were administered at 3-month intervals at the supraspinatus tear site, and tendon integrity was evaluated 6 months after the first injection using magnetic resonance imaging (MRI). The patients were divided into 2 groups: atelocollagen injection (group 1, n = 49) and ADM injection (group 2, n = 41). Supraspinatus tear size was measured in T2 coronal and sagittal views. Outcomes were categorized into 3 groups by tear size change from initial to final follow-up: improved (< 0-2 mm), no interval change (-2 to 2 mm), and worsened (> 2 mm). Clinical scores and range of motion (ROM) were measured in both groups. The atelocollagen group showed improved outcomes in 34.7% of the patients, whereas 55.1% and 10.2% showed no interval change and worsening in the coronal plane, respectively. The ADM group showed improved outcomes in 48.8% of the patients, whereas 48.8% and 2.4% showed no interval change and worsened results in the coronal plane, respectively. The mean change in tear size was -1.02 ± 2.87 mm for group 1 and -2.31 ± 3.62 mm for group 2 (p < 0.05). In the sagittal plane, 20.4% of the patients in group 1 showed improvement, 77.6% showed no interval change, and 2% showed worsened outcomes. Group 2 showed improvement in 31.7% of patients, 58.5% showed no interval change, and 9.8% showed worsened outcomes. Tear size changed by -0.56 ± 1.90 mm for group 1 and -0.8 ± 2.37 mm for group 2 (p > 0.05). No significant differences were noted in the ROM between the 2 groups at any time. Clinical scores also showed no significant differences between the 2 groups, except for the Constant Shoulder Score at the 3-month follow-up. Compared with atelocollagen injection, ADM injection resulted in a superior improvement in rotator cuff tendon integrity. However, clinical outcomes were comparable between the groups.

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A review on MMP-2 modulating agents from natural and synthetic sources and their role in inflammatory bowel disease.

Ragunath Murugasamy M, Ardra Sudarsan S, Balde Akshad A, Nazeer Rasool Abdul RA

Inflammatory bowel disease (IBD), encompassing Crohn's disease and ulcerative colitis, is characterized by chronic intestinal inflammation, epithelial barrier dysfunction, immune dysregulation, and aberrant extracellular matrix (ECM) remodeling. Matrix metalloproteinase-2 (MMP-2), a zinc-dependent gelatinase, has emerged as a critical regulator of intestinal homeostasis owing to its dual role in tissue repair and inflammatory tissue destruction. Unlike several inducible matrix metalloproteinases, MMP-2 is constitutively expressed and tightly regulated through interactions with membrane-type MMPs, tissue inhibitors of metalloproteinases (TIMPs), cytokines, redox signalling, and microbial factors. Dysregulated MMP-2 activity contributes to epithelial barrier disruption, leukocyte infiltration, chronic inflammation, fibrosis, and disease progression in IBD. This review summarizes the current understanding of MMP-2 biology, activation mechanisms, and immunopharmacological functions in intestinal inflammation, while critically evaluating therapeutic strategies aimed at its modulation. Particular emphasis is placed on natural and synthetic MMP-2 modulators, including animal-derived peptides and endogenous inhibitors, plant-derived polyphenols, flavonoids, alkaloids, terpenoids, and rationally designed small-molecule and peptidomimetic inhibitors. Emerging nanocarrier-based and targeted delivery systems are also discussed as approaches to enhance selectivity and minimize systemic toxicity. Furthermore, the review highlights the limitations of broad-spectrum MMP inhibition and underscores the need for site-specific modulation that preserves physiological tissue remodeling while suppressing pathological activity. Advances in precision medicine, single-cell and spatial transcriptomics, organoid-based disease models, and microbiome-informed therapeutic strategies are expected to facilitate the development of next-generation MMP-2-targeted interventions. Collectively, MMP-2 represents a promising yet complex therapeutic target whose successful modulation may improve long-term outcomes in IBD.

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