Zoptrex (zoptarelin doxorubicin) / COSCIENS Biopharma - LARVOL DELTA

Two GnRH-mitoxantrone Conjugates, Con-3 and Con-7, Target Endometrial Cancer Cells. (PubMed, Curr Mol Pharmacol) - "In contrast, the free, mitoxantrone-unconjugated peptides did not affect the proliferation of Ishikawa cells. The Con-3 and Con-7 could put the basis for the development of a new class of anticancer drugs for endometrial cancer, which will act as "prodrugs" that deliver the cytotoxic mitoxantrone in a GnRH-R-specific manner."

Journal • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor

Cytotoxic activity and cell specificity of a novel LHRH peptide drug conjugate, D-Cys6-LHRH vedotin, against ovarian cancer cell lines. (PubMed, Chem Biol Drug Des) - "A GI50 and cell specificity comparison against cancerous and non-cancerous ovarian cell lines showed significantly superior bioactivity and selectivity over Zoptarelin doxorubicin (GI50 4 vs. 453 nM) and other chemotherapeutic drugs used for treating ovarian cancers. Our results suggest D-Cys6-LHRH vedotin can potentially be used as a treatment for ovarian cancer."

Journal • Preclinical • Colorectal Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

A phase II trial of zoptarelin doxorubicin in castration- and taxane-resistant prostate cancer. (ASCO-GU 2017) - P1/2; "This phase 2 trial demonstrated clinical benefit in 56% of patients with no DLT or other toxicity requiring treatment termination. These results suggest a role for zoptarelin doxorubicin for mCRPC following progression on second- and third-line hormonal therapy."

Clinical • P2 data • Pain • Prostate Cancer

ZoptEC: Phase III randomized controlled study comparing zoptarelin with doxorubicin as second line therapy for locally advanced, recurrent, or metastatic endometrial cancer (NCT01767155). (ASCO 2018) - P3; "Zoptarelin did not improve OS, PFS, ORR, CBR, or adverse events compared to doxorubicin as second line therapy for advanced endometrial cancers."

Clinical • P3 data • Endometrial Cancer

The Role of Gonadotropin-Releasing Hormone (GnRH) in Endometrial Cancer. (PubMed, Cells) - "The cytotoxic GnRH-analog Zoptarelin Doxorubicin has shown encouraging activity in a phase II trial in patients with advanced or recurrent EC, which expressed GnRH-R. In a phase III trial in patients with EC of unknown GnRH-R expression, the cytotoxic GnRH doxorubicin conjugate was not superior to free doxorubicin. Further well-designed clinical trials exploiting the GnRH-system in EC might be useful."

Journal • Review • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor

ZoptEC: Zoptarelin Doxorubicin (AEZS 108) as Second Line Therapy for Endometrial Cancer (clinicaltrials.gov) - P3; N=512; Completed; Sponsor: AEterna Zentaris; Active, not recruiting ➔ Completed

Trial completion • Biosimilar • Endometrial Cancer • Oncology • Uterine Cancer

Study Comparing AEZS-108/ZoptEC (Zoptarelin Doxorubicin in Endometrial Cancer) to Doxorubicin as a Second Line Therapy of Endometrial Cancer (clinicaltrials.gov) - P3; N=500; Recruiting; Sponsor: AEterna Zentaris

Trial completion date • Biosimilar • Oncology

Zoptarelin Doxorubicin (AEZS 108) as Second Line Therapy for Endometrial Cancer (clinicaltrials.gov) - P3; N=500; Active, not recruiting; Sponsor: AEterna Zentaris; Recruiting -> Active, not recruiting ; Trial primary completion date: Dec 2015 ->Dec 2016

Enrollment closed • Trial primary completion date • Biosimilar • Oncology • Uterine Cancer

The targeted LHRH analog AEZS-108 alters expression of genes related to angiogenesis and development of metastasis in uveal melanoma. (PubMed, Oncotarget) - "AEZS-108 is a hybrid molecule, composed of a synthetic peptide carrier and the cytotoxic doxorubicin (DOX). In conclusion, we show for the first time that AEZS-108 has a major impact in the regulation of angiogenesis thus plays a potential role in tumor suppression. Taken together, our results support the development of novel therapeutic strategies for UM focusing on LHRH receptors."

Journal • HIF1A • SERPINB5

Inhibition of aerobic glycolysis enhances the anti-tumor efficacy of Zoptarelin Doxorubicin in triple-negative breast cancer cells. (PubMed, J Obstet Gynaecol Res) - "The glycolytic phenotype of TNBC can be used to improve antitumor therapies. Co-treatment of Zoptarelin Doxorubicin with glycolysis inhibitor 2DG might be a suitable therapeutic option for GnRH receptor-positive TNBC."

Clinical • Journal