afimoxifene / Besins Healthcare - LARVOL DELTA

Testing an Active Form of Tamoxifen (4-hydroxytamoxifen) Delivered Through Breast Skin to Control Ductal Carcinoma in Situ (DCIS) of the Breast (clinicaltrials.gov) - P2 | N=100 | Completed | Sponsor: Northwestern University | Recruiting ➔ Completed | Phase classification: P2b ➔ P2

Phase classification • Trial completion • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2 | N=194 | Completed | Sponsor: M.D. Anderson Cancer Center | Active, not recruiting ➔ Completed

Trial completion • Breast Cancer • Oncology • Solid Tumor

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2 | N=194 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial completion date: Apr 2023 ➔ Oct 2023 | Trial primary completion date: Apr 2023 ➔ Oct 2023

Trial completion date • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor • AURKA • CD68

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2 | N=156 | Recruiting | Sponsor: Northwestern University | Suspended ➔ Recruiting | N=120 ➔ 156

Enrollment change • Enrollment open • Breast Cancer • Oncology • Solid Tumor

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2 | N=120 | Suspended | Sponsor: Northwestern University | Trial primary completion date: Jun 2023 ➔ Jan 2024

Trial primary completion date • Breast Cancer • Oncology • Solid Tumor

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2 | N=194 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial primary completion date: Oct 2021 ➔ Apr 2023

Trial primary completion date • Breast Cancer • Oncology • Solid Tumor • AURKA • CD68

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2 | N=120 | Suspended | Sponsor: Northwestern University | Trial completion date: Jun 2023 ➔ Jun 2024 | Recruiting ➔ Suspended | Trial primary completion date: Jun 2022 ➔ Jun 2023

Trial completion date • Trial primary completion date • Trial suspension • Breast Cancer • Oncology • Solid Tumor

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2 | N=152 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial primary completion date: Apr 2023 ➔ Oct 2021

Trial primary completion date • Breast Cancer • Oncology • Solid Tumor • AURKA • CD68

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2 | N=152 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial completion date: Oct 2021 ➔ Apr 2023 | Trial primary completion date: Oct 2021 ➔ Apr 2023

Trial completion date • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor • AURKA • CD68

Evaluation of human adipose-derived stromal cell behaviour following exposure to Tamoxifen. (PubMed, Tissue Cell) - "At physiologically relevant doses, Tamoxifen treatment did not result in any deleterious effect on ASC survival and functionality and is unlikely to negatively impact ASC based breast reconstruction strategies for breast cancer patients receiving this adjuvant hormonal therapy."

Journal • Aesthetic Medicine • Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2; N=152; Active, not recruiting; Sponsor: M.D. Anderson Cancer Center; Recruiting ➔ Active, not recruiting; Trial completion date: Sep 2022 ➔ Oct 2021

Clinical • Enrollment closed • Trial completion date • Breast Cancer • Oncology • Solid Tumor • AURKA • CD68

Testing an Active Form of Tamoxifen (4-hydroxytamoxifen) Delivered Through the Breast Skin to Control Ductal Carcinoma in Situ (DCIS) of the Breast (clinicaltrials.gov) - P2b; N=100; Recruiting; Sponsor: Northwestern University; Trial completion date: Jul 2019 ➔ Jul 2023; Trial primary completion date: Jul 2019 ➔ Jul 2022

Clinical • Trial completion date • Trial primary completion date • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CD68 • ER • IGF1

Testing an Active Form of Tamoxifen (4-hydroxytamoxifen) Delivered Through the Breast Skin to Control Ductal Carcinoma in Situ (DCIS) of the Breast (clinicaltrials.gov) - P2b; N=100; Not yet recruiting; Sponsor: National Cancer Institute (NCI)

Clinical • New P2b trial • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CD68 • ER • IGF1

Testing an Active Form of Tamoxifen (4-hydroxytamoxifen) Delivered Through the Breast Skin to Control Ductal Carcinoma in Situ (DCIS) of the Breast (clinicaltrials.gov) - P2b; N=100; Not yet recruiting; Sponsor: Northwestern University; Initiation date: Mar 2017 ➔ Jun 2017

Clinical • Trial initiation date • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CD68 • ER • IGF1

Testing an Active Form of Tamoxifen (4-hydroxytamoxifen) Delivered Through the Breast Skin to Control Ductal Carcinoma in Situ (DCIS) of the Breast (clinicaltrials.gov) - P2b; N=100; Recruiting; Sponsor: Northwestern University; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • CD68 • ER • IGF1

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2; N=152; Recruiting; Sponsor: M.D. Anderson Cancer Center; Trial completion date: Sep 2020 ➔ Sep 2022; Trial primary completion date: Sep 2020 ➔ Sep 2021

Clinical • Trial completion date • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor • CD68

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2; N=120; Recruiting; Sponsor: Northwestern University; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Breast Cancer • Oncology • Solid Tumor

Elucidating Binding Sites and Affinities of ERα Agonists and Antagonists to Human Alpha-Fetoprotein by In Silico Modeling and Point Mutagenesis. (PubMed, Int J Mol Sci) - "In our study, we constructed a homology-based 3D model of human AFP (HAFP) with the purpose of molecular docking of ERα ligands, three agonists (17β-estradiol, estrone and diethylstilbestrol), and three antagonists (tamoxifen, afimoxifene and endoxifen) into the obtained structure. We performed in silico point substitutions of amino acid residues to confirm their roles in HAFP-ligand interactions and showed that Thr132, Leu138, His170, Phe172, Ser217, Gln221, His266, His316, Lys453, and Asp478 residues, along with two disulfide bonds (Cys224-Cys270 and Cys269-Cys277), have key roles in both HAFP-estrogen and HAFP-antiestrogen binding. Data obtained in our study contribute to understanding mechanisms underlying protein-ligand interactions and anticancer therapy strategies based on ERα-binding ligands."

Journal • Oncology

Synthesis of Tamoxifen-Artemisinin and Estrogen-Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer. (PubMed, ChemMedChem) - "Most of the hybrid compounds exhibit a strong anti-cancer activity against both cancer cell lines e.g., EC 50 (PC-3) down to 1.07 µM and EC 50 (MCF-7) down to 2.08 µM, thus showing higher activities than their parent compounds 4-hydroxytamoxifen (Afimoxifene, 7 ) (EC 50 (PC-3) = 75.1 µM and EC 50 (MCF-7) = 19.3 µM), dihydroartemisinin ( 2 ) (EC 50 (PC-3) = 263.6 µM and EC 50 (MCF-7) = 49.3 µM) and artesunic acid ( 3 ) (EC 50 (PC-3) = 195.1 µM and EC 50 (MCF-7) = 32.0 µM). The most potent compounds were the estrogen-artemisinin hybrids 27 and 28 (EC 50 (PC-3) = 1.18 µM and 1.07 µM, correspondingly) against prostate cancer and hybrid 23 (EC 50 (MCF-7) = 2.08 µM) against breast cancer. These findings demonstrate the high potential of hybridization of artemisinin and estrogens to further improve their anticancer activities and to produce synergistic effects between linked pharmacophores."

Journal

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2; N=120; Not yet recruiting; Sponsor: Northwestern University; Initiation date: Jul 2019 ➔ Jan 2020

Clinical • Trial initiation date

Low dose tamoxifen and other approaches to improve chemoprevention uptake (SABCS 2019) - "The use of transdermal 4-OH tamoxifen (afimoxifene) gel is also being actively pursued in clinical trials. Initial findings indicate the feasibility of this approach in attaining active concentrations in the breast and modulation of Ki-67 (Lee et al Cancer Chemother Pharmacol. 2015)."

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2; N=152; Recruiting; Sponsor: M.D. Anderson Cancer Center; Trial primary completion date: Sep 2019 ➔ Sep 2020

Clinical • Trial primary completion date

Topical Afimoxifene in Treating Patients With Breast Cancer Who Have Undergone Radiation Therapy on One Breast (clinicaltrials.gov) - P2; N=120; Not yet recruiting; Sponsor: Northwestern University

Clinical • New P2 trial

Afimoxifene in Reducing the Risk of Breast Cancer in Women With Mammographically Dense Breast (clinicaltrials.gov) - P2; N=152; Recruiting; Sponsor: M.D. Anderson Cancer Center; Trial completion date: May 2019 ➔ Sep 2020; Trial primary completion date: May 2019 ➔ Sep 2019

Clinical • Trial completion date • Trial primary completion date