AVZO-021 / Allorion Therap, Avenzo Therap - LARVOL DELTA

ARTS-023: a potent and selective CDK4 Inhibitor demonstrating anti-tumor activity in preclinical ER+ breast cancer models (AACR 2025) - "Additionally, it demonstrated robust synergistic effects when combined with the CDK2 inhibitor AVZO-021 in both palbociclib-sensitive cell line-derived xenograft models and palbociclib-resistant patient-derived xenograft models. Taken together, these findings establish ARTS-023 as a promising next-generation CDK4-selective inhibitor, offering improved efficacy and reduced toxicity for patients with ER+ breast cancer. Furthermore, the favorable toxicity profile of ARTS-023 supports the potential combination with CDK2 inhibitors to enhance therapeutic outcomes."

Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CCND1 • ER • HER-2

AVZO-021-1001: A first-in-human open-label, multicenter phase I/II dose-escalation and expansion study evaluating AVZO-021 in adult patients with advanced solid tumors (ESMO 2024) - P1/2 | "Combination dose-escalation will be initiated with fulvestrant and current CDK4/6 inhibitors (Part 1b) in patients with HR+/HER2- mBC, and an additional combination with carboplatin (Part 1c) in patients with CCNE1-amplified metastatic endometrial ovarian cancer (EOC). Secondary endpoints are DOR, PFS, OS, PK, and safety; exploratory endpoints include PD and biomarker analyses. The trial is ongoing and plans to enroll patients at ∼50 centers across the US, Europe, and Australia."

Clinical • Metastases • P1/2 data • Breast Cancer • Endometrial Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • CCNE1 • CDK1 • HER-2 • PKMYT1

Avenzo Therapeutics Announces Clinical Study Collaboration with Gilead Sciences to Evaluate AVZO-021 and Trodelvy in HR+/HER2- Metastatic Breast Cancer (Businesswire) - "Avenzo Therapeutics...announced it has entered into a clinical study collaboration and supply agreement with Gilead Sciences, Inc...to evaluate the safety and efficacy of AVZO-021, its investigational, potentially best-in-class CDK2 inhibitor, in combination with Gilead’s Trodelvy (sacituzumab govitecan-hziy), a Trop-2 directed antibody-drug conjugate (ADC), as a potential treatment for patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer...'We look forward to initiating combination cohorts with Trodelvy, as well as CDK4/6 inhibitors, in the Phase 1b portion of the ongoing clinical study in the fourth quarter of 2024.'....Under the clinical study collaboration and supply agreement, Gilead will provide Trodelvy to Avenzo, who will conduct and sponsor the combination study. Avenzo and Gilead will retain all development and commercial rights to their respective compounds...'"

Licensing / partnership • Trial status • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

ARTS-021-1001: Study of AVZO-021 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=430 | Recruiting | Sponsor: Avenzo Therapeutics, Inc. | N=192 ➔ 430 | Trial completion date: Apr 2026 ➔ Jan 2030 | Trial primary completion date: Oct 2025 ➔ Jan 2028

Combination therapy • Enrollment change • Metastases • Trial completion date • Trial primary completion date • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CCNE1 • HER-2

Avenzo Therapeutics Announces $150 Million Oversubscribed Financing To Advance Emerging Oncology Pipeline (Businesswire) - "Avenzo Therapeutics, Inc...announced the closing of an oversubscribed $150 million Series A-1 financing. The total capital raised since the company’s founding in August 2022 is $347 million....Proceeds from the financing will be used to advance Avenzo’s emerging oncology pipeline which is led by AVZO-021, a potentially best-in-class cyclin-dependent kinase 2 (CDK2) selective inhibitor being studied in an ongoing U.S.-based Phase 1 clinical study for the treatment of HR+/HER2- metastatic breast cancer and other advanced solid tumors."

Financing • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

Avenzo Therapeutics Announces Global License of AVZO-021 (ARTS-021), a Potentially Best-in-Class Clinical Stage CDK2 Inhibitor from Allorion Therapeutics (Businesswire) - "Avenzo Therapeutics, Inc...today announced that it has entered into an exclusive licensing agreement with Allorion Therapeutics Inc. (Allorion) to develop and commercialize AVZO-021 (formerly ARTS-021), a potentially best-in-class cyclin-dependent kinase 2 (CDK2) selective inhibitor globally (excluding Greater China). As part of the agreement, Avenzo also receives an exclusive option for an additional preclinical program planned for IND submission in early 2025...'AVZO-021 may provide patients with a new treatment option both as a single agent and in multiple combinations. We are excited to advance the ongoing Phase 1 clinical study (NCT05867251), and to partner with the Allorion team to advance the program globally.'...Under the terms of the license agreement, Allorion will receive an upfront payment of $40 million..."

Licensing / partnership • Trial status • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

ARTS-021-1001: Phase I/II study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors (ESMO 2023) - "Trial design This is a first in human, open label, multicenter phase1/2 dose escalation and dose expansion study to evaluate the safety, tolerability, PK, PD, and anti-tumor activity of ARTS-021 1) as a single agent in advanced or metastatic CCNE-1 amplifed solid tumors; 2) in combination with Carboplatin to treat refractory/resistant CCNE-1 amplified ovarian cancer that has failed standard therapies; 3) in combination with endocrine therapy (fulvestrant/letrozole) and CDK4/6 inhibitor(palbociclib/ribociclib/abemaciclib) to treat HR+ HER2- breast cancer patients have failed standard therapies. The secondary endpoint of phase 2 study will be safety/tolerability. Archival tumor and paired fresh tumor biopsy will be collected throughout the study for exploratory pharmacodynamics (PD) and biomarker evaluation."

Metastases • P1/2 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • CCNE1 • CDK1 • HER-2

ALLORION THERAPEUTICS ANNOUNCES FIRST PATIENT DOSED IN PHASE 1/2 STUDY OF ARTS-021, A POTENTIAL BEST IN CLASS CDK2 INHIBITOR, FOR ADVANCED OR METASTATIC SOLID TUMORS (Canada Newswire) - "Allorion Therapeutics...announced today the dosing of its first patient in the Phase 1/2 trial of ARTS-021....This open-label, first-in-human study is currently ongoing in the US and is designed to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and efficacy of ARTS-021 in adult patients with advanced or metastatic solid tumors."

Trial status • Oncology • Solid Tumor

Study of ARTS-021 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=192 | Recruiting | Sponsor: Allorion Therapeutics Inc | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Metastases • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CCNE1 • HER-2

Phase 1/2 study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors. (ASCO 2023) - "Furthermore, consistent with the hypothesis that CDK2 activity may mediate resistance to CDK4/6 inhibitors, ARTS-021 significantly enhanced Palbociclib anti-tumor activity in an estrogen positive (ER+) breast cancer xenograft model... A first in human, open label, multicenter phase1/2 dose escalation and dose expansion study will be conducted to evaluate the safety, tolerability, PK, pharmacodynamics (PD), and anti-tumor activity of ARTS-021 1) as a single agent in advanced or metastatic solid tumors harboring CCNE-1 gene amplification; 2) in combination with carboplatin to treat refractory/resistant CCNE-1 amplified ovarian cancer that has failed standard therapies; 3) in combination with endocrine therapy and CDK4/6 inhibitor to treat ER+/HER2- breast cancer patients have failed standard therapies... ARTS-021 shows potential anti-tumor activities."

Metastases • P1/2 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • CCNE1 • CDK1 • ER • HER-2

Study of ARTS-021 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=192 | Not yet recruiting | Sponsor: Allorion Therapeutics Inc

Combination therapy • Metastases • New P1/2 trial • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CCNE1 • HER-2

Allorion Therapeutics, a next-generation precision medicine company focusing on oncology and autoimmune diseases, raises $50 million Series B financing (PRNewswire) - "Allorion Therapeutics...announces the completion of a $50 million Series B financing round, co-led by INCE Capital and Qiming Venture Partners, with participation from TF Capital, Long River Investment (LRI), 3SBio, Octagon Capital, and Elikon Venture....The funds raised in this round will primarily support upcoming Phase I/II clinical trials in both China and the U.S. and the identification of clinical candidates for additional programs....ARTS-021, with its IND to be filed in the U.S. and China shortly, is a highly potent CDK2 isoform selective inhibitor for treatment of solid tumors such as ovarian, endometrial, and breast cancer."

Financing • New P1/2 trial • Breast Cancer • Endometrial Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor • Uterine Cancer