Cantrixil (TRX-E-002-1) / Yale University, Kazia, Vivesto - LARVOL DELTA

Kazia Therapeutics Announces Sale of Intellectual Property and Trademarks Rights for Cantrixil (PRNewswire) - "Kazia Therapeutics Limited...an oncology-focused drug development company, today announced the sale of all intellectual property and trademarks rights to Cantrixil for USD $1 million....In March 2021, Vivesto licensed the exclusive global development and commercialization rights for Cantrixil from Kazia Therapeutics. Having decided not to pursue development of Cantrixil in ovarian cancer, as originally anticipated under the license, Vivesto is currently exploring Cantrixil preclinically for the treatment of hematological cancers."

Commercial • Hematological Malignancies • Ovarian Cancer

Vivesto reports positive Cantrixil results in an animal hematological cancer model (Vivesto Press Release) - "Vivesto AB...today announced that positive preclinical efficacy data was obtained in an animal model of hematological cancer. The results support continued development of the candidate drug Cantrixil within this indication and are in line with previous positive preclinical data....The experimental trial demonstrates, for the first time, that Cantrixil can reduce tumor growth and increase survival times in a well-established mouse model of hematological cancer. The treatment was well tolerated and safe."

Preclinical • Hematological Malignancies

Vivesto reports positive preclinical data supporting continued development of Cantrixil (Vivesto Press Release) - "Vivesto AB...today announced that positive preclinical data was obtained supporting continued development of the candidate drug Cantrixil within the indications bladder and blood cancer. The data indicates that Cantrixil has suitable drug properties and an acceptable safety profile, with minimal unwanted effects...Data from ADME studies (Absorption, Distribution, Metabolism, and Excretion) and secondary pharmacology studies confirm that Cantrixil has suitable physicochemical properties and an acceptable safety profile with minimal off-target effects, supporting continued development in bladder and blood cancer indications. Additional in vitro and in vivo studies are planned during 2024 to ensure the properties, safety and efficacy of the drug before proceeding to clinical trials."

PK/PD data • Preclinical • Bladder Cancer • Genito-urinary Cancer • Hematological Malignancies • Oncology • Solid Tumor

[VIRTUAL] TRX-E-002-1 in treatment-refractory ovarian cancer - 3-month follow-up results from a phase I study dose escalation phase (AACR-II 2020) - P1 | "IP administered TRX-E-002-1 as a first-in-class, dual acting, anti-cancer therapy has preliminary activity for the treatment of platinum resistant ovarian cancer for patients who have demonstrated resistance to a range of prior treatments."

P1 data • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor • CA125 • CD44

Phase I study of intraperitoneal TRX-E-002-1 in subjects with persistent or recurrent ovarian, fallopian tube or primary peritoneal cancer: Three-month follow-up results of the dose escalation phase (ESMO 2019) - P1; "IP administered TRX-E-002-1 as a first-in-class, dual acting, anti-cancer therapy has demonstrated preliminary activity for the treatment of platinum resistant ovarian cancer. Clinical trial identification: NCT02903771. Legal entity responsible for the study: Kazia Therapeutics Limited."

Clinical • P1 data

[VIRTUAL] TRX-E-002-1 in treatment-refractory ovarian cancer: Final phase 1 study results from the dose-escalation and dose-expansion cohorts (AACR 2021) - P1 | "IP-administered Cantrixil, a first-in-class, dual acting, anti-cancer therapy has encouraging activity in a cohort of difficult to treat patients with persistent epithelial ovarian, fallopian tube or primary peritoneal cancer who have demonstrated resistance to a range of prior treatments. Disease response compares favorably to a figure of 10% for historical controls."

P1 data • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor

Maximum Tolerated Dose and Anti-Tumor Activity of Intraperitoneal Cantrixil (TRX-E-002-1) in Patients with Persistent or Recurrent Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer: Phase I Study Results. (PubMed, Cancers (Basel)) - P1 | "The molecular target and mechanism of action of Cantrixil are yet to be confirmed. Preliminary analysis of stem cell markers suggests that IP Cantrixil might induce ovarian cancer stem cell death and sensitize cells to standard chemotherapy, warranting further evaluation."

Clinical • Journal • P1 data • Fallopian Tube Cancer • Gastrointestinal Disorder • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor

Kazia Licenses Cantrixil, a Clinical-stage, First-in-class Ovarian Cancer Drug Candidate, to Oasmia Pharmacetical AB (PRNewswire) - "Kazia Therapeutics Limited...is pleased to announce that it has entered into an exclusive worldwide license agreement with Oasmia Pharmaceutical AB (STO: OASM), an innovation-focused specialty pharmaceutical company, for Cantrixil (TRX-E-002-1), a clinical-stage, first-in-class drug candidate under development for the treatment of ovarian cancer...Oasmia will assume worldwide exclusive rights to develop and commercialise Cantrixil for all indications, with an initial focus on ovarian cancer...Oasmia expects to commence a Phase II study of Cantrixil in ovarian cancer in 2022."

Licensing / partnership • New P2 trial • Genito-urinary Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer

Top-line Final Data from Cantrixil Phase I Study Confirms Prior Positive Efficacy and Safety Signals (PRNewswire) - P1, N=28; NCT02903771; Sponsor: Kazia Therapeutics Limited; "Kazia Therapeutics Limited...is pleased to share top-line final data from its phase I study of Cantrixil (TRX-E-002-1) in patients with persistent or recurrent ovarian cancer...Trial achieved its primary objective, determining the maximum tolerated dose (MTD) of Cantrixil to be 5 mg/kg; Overall, 16 patients were evaluable for efficacy. One patient demonstrated a complete response (CR) and two patients experienced a partial response (PR), according to industry-standard RECIST criteria, making an overall response rate (ORR) of 19%...Kazia expects the full data to be presented at a suitable academic conference and published in a peer-reviewed journal in 1H CY2021."

P1 data • Gynecologic Cancers • Oncology • Ovarian Cancer

Kazia Presents Further Paxalisib and Cantrixil Data at AACR, Reinforcing Positive Efficacy Signals for both Drugs (PRNewswire) - P1, N=28; NCT02903771; Sponsor: Kazia Therapeutics Limited; "Cantrixil data shows one complete response (CR) to treatment, meaning no measurable disease, and two partial responses (PR), for an overall response rate of 19% (3 / 16 evaluable patients)"

P1 data • Oncology • Ovarian Cancer

Phase I Study of Cantrixil in Patients With Ovarian Cancer, Fallopian Tube Cancer or Primary Peritoneal Cancer. (clinicaltrials.gov) - P1; N=28; Completed; Sponsor: Kazia Therapeutics Limited; Active, not recruiting ➔ Completed; Trial primary completion date: Dec 2019 ➔ Mar 2020

Clinical • Trial completion • Trial primary completion date • Breast Cancer • Fallopian Tube Cancer • Gynecologic Cancers • Hematological Disorders • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor • BRCA • CA125

Mechanism of action of the third generation benzopyrans and evaluation of their broad anti-cancer activity in vitro and in vivo. (PubMed, Sci Rep) - "In this study, we investigated the mechanism of action of the third-generation benzopyran compounds, TRX-E-002-1 and TRX-E-009-1...This finding along with immunostaining, in vitro polymerization assays, and animal experiments in both athymic and immunocompetent mice, demonstrates that these third-generation benzopyran compounds are potent tubulin polymerization inhibitors in vitro and in vivo, and this is the molecular basis of their anti-cancer activity in melanoma. These findings indicate these BP compounds may offer a novel anti-microtubule strategy for cancer intervention and provides the basis for further investigation into biomarkers of clinical sensitivity."

Biomarker • Journal • Preclinical

Phase I Study of Cantrixil in Patients With Ovarian Cancer, Fallopian Tube Cancer or Primary Peritoneal Cancer. (clinicaltrials.gov) - P1; N=28; Active, not recruiting; Sponsor: Kazia Therapeutics Limited; Recruiting ➔ Active, not recruiting; N=60 ➔ 28; Trial completion date: Dec 2019 ➔ Mar 2020

Clinical • Enrollment change • Enrollment closed • Trial completion date

Kazia presents positive Cantrixil phase I data at AACR conference (PRNewswire) - P1, N=60; NCT02903771; Sponsor: Kazia Therapeutics; "A Maximum Tolerated Dose (MTD) of 5mg/kg was determined. This is well within the predicted therapeutic range, based on preclinical data, and supports moving forward with subsequent clinical development. Of nine patients evaluable for efficacy, five (56%) achieved stable disease after two cycles of Cantrixil monotherapy. One of these five patients subsequently achieved a partial response when Cantrixil was administered with chemotherapy...An expansion cohort is currently underway to seek efficacy signals, and is planned to enroll 12 patients, all of whom will receive a dose of 5 mg/kg; initial data from this cohort is expected in 2H of calendar 2019."

P1 data

Kazia to present on Cantrixil at American Association for Cancer Research (AACR) 2019 Annual Meeting (PRNewswire) - "Australian oncology-focused biotech company Kazia Therapeutics Ltd...has been selected to present data from the Phase I study of Cantrixil in ovarian cancer at the American Association for Cancer Research (AACR) 2019 Annual Meeting."

P1 data