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

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

Avenzo Therapeutics…reported updated clinical data from the Phase 1 portion of its ongoing Phase 1/2 clinical study of AVZO-021, its potentially differentiated cyclin-dependent kinase 2 (CDK2) selective inhibitor (Businesswire) - "The updated data demonstrated clinical activity in heavily pretreated patients with hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer. Across all monotherapy doses, median progression-free survival (PFS) for all HR+/HER2- breast cancer patients, with a median of 4.0 (min, max: 1, 9) prior lines of therapies in the metastatic setting, was 5.3 months. Consistent with previously reported findings, AVZO-021 was generally well tolerated with relatively low incidence and severity of gastrointestinal and hematologic adverse events, which are commonly observed adverse events associated with less selective CDK inhibitors. The findings were reported at the 2026 American Society of Clinical Oncology Annual Meeting."

P1 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Rallybio Corporation and Avenzo Therapeutics Announce Merger Agreement to Advance Next-Generation Oncology Therapies and $215 Million Concurrent Private Placement (Businesswire) - "Upon completion of the Merger, the combined company is expected to operate under the name Avenzo Therapeutics....The combined company expects its cash balance at closing to fund operations into late 2028 and support advancement of its four clinical-stage programs through multiple clinical milestones."

M&A • Solid Tumor

A phase 1/2, first-in-human study of AVZO-021, a selective cyclin-dependent kinase 2 inhibitor (CDK2i), as monotherapy and in combination for patients with advanced solid tumors, including hormone receptor–positive (HR+)/human epidermal growth factor receptor 2–negative (HER2−) breast cancer (BC) and cyclin E1 (CCNE1)–amplified solid tumors: Updated safety and efficacy results. (ASCO 2026) - P1/2 | "With longer follow-up, AVZO-021 as monotherapy and in combination with fulvestrant continues to show an encouraging tolerability profile and clinically meaningful efficacy. Gastrointestinal and hematologic adverse events continue to be of low incidence and severity allowing for prolonged treatment and potential safe combination with AVZO-023, a highly potent and selective CDK4i currently enrolling patients with HR+/HER2- BC in combination with fulvestrant."

Clinical • First-in-human • Metastases • Monotherapy • P1/2 data • Breast Cancer • Endometrial Cancer • Fallopian Tube Cancer • Gastrointestinal Disorder • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Neutropenia • Oncology • Ovarian Cancer • Solid Tumor • Uterine Cancer • CCNE1 • CDK1 • CDK4 • CDKN2A • HER-2

Avenzo Therapeutics Announces First Patient Dosed in Combination Cohort Evaluating CDK4 Selective Inhibitor (AVZO-023) with CDK2 Selective Inhibitor (AVZO-021) In Ongoing Phase 1/2 ORION-1 Study (Businesswire) - "The Phase 1/2 first-in-human, open-label ORION-1 clinical study is designed to assess the safety, tolerability, and preliminary clinical activity of AVZO-023 with endocrine therapy as well as the combination of AVZO-023 and AVZO-021 with endocrine therapy. The combination cohort will evaluate AVZO-023 and AVZO-021 with fulvestrant in patients with HR+/HER2- advanced or metastatic breast cancer."

First-in-human • Trial status • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Avenzo Therapeutics Advances the Combination of CDK4 Selective Inhibitor (AVZO-023) with CDK2 Selective Inhibitor (AVZO-021) in Ongoing Phase 1/2 ORION-1 Study in HR+/HER2- Breast Cancer (Businesswire) - "The Phase 1/2 first-in-human, open-label ORION-1 clinical study is designed to assess the safety, tolerability, and preliminary clinical activity of AVZO-023 with endocrine therapy as well as the combination of AVZO-023 and AVZO-021 with endocrine therapy. The combination cohort will evaluate AVZO-023 and AVZO-021 with fulvestrant in patients with HR+/HER2- metastatic breast cancer."

First-in-human • Trial status • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Avenzo Therapeutics to Present Updated Results from the Phase 1 Study of AVZO-021, a Potential Best-in-Class CDK2 Inhibitor, at the 2026 American Society of Clinical Oncology Annual Meeting (Businesswire) - "Avenzo will present updated safety and efficacy results from the Phase 1 portion of its ongoing Phase 1/2 clinical study of AVZO-021..."

P1 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Solid Tumor

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

A phase 1/2 study of AVZO-023, a next-generation selective cyclin-dependent kinase 4 inhibitor (CDK4i), as a single agent and in combination with AVZO-021, a selective cyclin-dependent kinase 2 inhibitor (CDK2i), and/or endocrine therapy in patients with advanced solid tumors (SABCS 2025) - P1/2 | "AVZO-023 showed strong anti-tumor activity in vivo, which was further enhanced in combination with the selective CDK2i AVZO-021 in palbociclib-sensitive and palbociclib-resistant xenograft models.Trial DesignThis Phase 1 AVZO-023-1001 trial (NCT06998407) will assess the safety, pharmacokinetics (PK), pharmacodynamics (PD), and anti-tumor activity of AVZO-023 as a single agent and in combination with endocrine therapy and/or AVZO-021...Patients with HR+/HER2- BC enrolled in Parts A or B will have the option to add fulvestrant to their study treatment. Part C will study the combination of AVZO-023 + letrozole ± AVZO-021...Primary objectives are safety/tolerability and secondary objectives include preliminary anti-tumor activity. The trial has activated and will enroll patients at approximately 50 centers across North America, Europe and the Asia-Pacific region."

Clinical • Combination therapy • Metastases • P1/2 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • CDK2 • CDKN2A • HER-2

A phase 1/2, first-in-human study of AVZO-021, a selective cyclin-dependent kinase 2 inhibitor (CDK2i), as a monotherapy and in combination for patients with advanced solid tumors, including hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer and cyclin E1 (CCNE1)‑amplified solid tumors: preliminary safety and efficacy results (SABCS 2025) - P1/2 | "We present preliminary results from the Phase 1 segment of the ongoing first-in-human Phase 1/2 study of AVZO-021 (NCT05867251). The ongoing Phase 1 open-label, dose-escalation segment of this study is evaluating the safety, pharmacokinetics (PK), and preliminary efficacy of AVZO-021 alone and in combination with endocrine therapy [(ET) fulvestrant], CDK4/6i (ribociclib/abemaciclib) + ET (fulvestrant/letrozole), an antibody-drug conjugate (sacituzumab govitecan-hziy), or chemotherapy (carboplatin) in patients with advanced solid tumors, including HR+/HER2− mBC and CCNE1-amplified solid tumors. AVZO-021 is a novel CDK2i with high selectivity for CDK2 over CDK1 and a favorable preliminary clinical profile. Together with the mechanistic rationale, the emerging clinical data support the continued development of AVZO-021 as a monotherapy and in combinations, including with ET ± CDK4/6i and selective CDK4i."

Clinical • First-in-human • Metastases • Monotherapy • P1/2 data • 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 • CCNE1 • CDK1 • CDKN2A • HER-2

Avenzo Therapeutics Presents Initial Results from the Phase 1/2 Study of AVZO-021, a Potential Best-in-Class CDK2 Inhibitor, at the 2025 San Antonio Breast Cancer Symposium (Businesswire) - "Of 19 efficacy-evaluable patients treated with AVZO-021 monotherapy, three patients experienced confirmed responses, including two with HR+/HER2- breast cancer with onset at weeks 15 and 36 and one with CCNE1-amplified ovarian cancer with onset at week 35....Of nine efficacy evaluable HR+/HER2- breast cancer patients treated with AVZO-021 in combination with fulvestrant, one patient experienced a confirmed response, with onset at week 7; the confirmatory scan was obtained after the data cut-off date."

P1/2 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Ovarian Cancer

…The company presented the study design for the ongoing Phase 1/2 study evaluating AVZO-023, its potential best-in-class cyclin-dependent kinase 4 (CDK4) selective inhibitor, as a single agent and in combination with AVZO-021 and/or endocrine therapy at the 2025 San Antonio Breast Cancer Symposium (Businesswire)

Clinical protocol • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Avenzo Therapeutics Announces $60 Million Series B Financing (Businesswire) - "The proceeds will be used to support the advancement of Avenzo’s pipeline of potential best-in-class oncology drug candidates."

Financing • Hormone Receptor Positive Breast Cancer • Non Small Cell Lung Cancer • Urothelial Cancer

Avenzo Therapeutics to Present Initial Results from the Phase 1 Study of AVZO-021, a Potential Best-in-Class CDK2 Inhibitor, at the 2025 San Antonio Breast Cancer Symposium (Businesswire) - "Avenzo will present preliminary safety and efficacy results from the Phase 1 portion of its ongoing Phase 1/2 clinical study of AVZO-021, its potential best-in-class cyclin-dependent kinase 2 (CDK2) selective inhibitor. The company will also highlight the Phase 1/2 study design evaluating AVZO-023...as a single agent and in combination with AVZO-021 and/or endocrine therapy."

Clinical protocol • P1 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Study of AVZO-023 as a Single Agent and in Combination With AVZO-021, and/or Endocrine Therapy in Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=380 | Recruiting | Sponsor: Avenzo Therapeutics, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

Avenzo Therapeutics Initiates Phase 1/2 Clinical Study of AVZO-023, a Potential Best-in-Class, Novel CDK4 Selective Inhibitor (Businesswire) - "Avenzo Therapeutics...announced initiation of a Phase 1/2 clinical study of its potential best-in-class cyclin-dependent kinase 4 (CDK4) selective inhibitor, AVZO-023, in patients with advanced or metastatic hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer and select other advanced solid tumors....The Phase 1/2 first-in-human, open-label clinical study is designed to assess the safety, tolerability, and preliminary clinical activity of AVZO-023 as a single agent and in combination with endocrine therapy and with AVZO-021, Avenzo’s potential best-in-class CDK2 inhibitor."

Trial status • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Study of AVZO-023 as a Single Agent and in Combination With AVZO-021, and/or Endocrine Therapy in Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=380 | Not yet recruiting | Sponsor: Avenzo Therapeutics, Inc.

New P1/2 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor

Avenzo Therapeutics Announces FDA Clearance of Investigational New Drug Application for AVZO-023 (ARTS-023), a Potential Best-in-Class, Novel CDK4 Selective Inhibitor (Businesswire) - "Avenzo Therapeutics...announced clearance by the U.S. Food and Drug Administration (FDA) of its investigational new drug application (IND) for AVZO-023 (formerly ARTS-023), a potential best-in-class, novel cyclin-dependent kinase 4 (CDK4) selective inhibitor. Avenzo has also exercised its exclusive option for AVZO-023 from Allorion Therapeutics Inc., securing global (excluding Greater China) development, manufacturing, and commercialization rights. Under the IND, the company plans to initiate a Phase 1/2 first-in-human, open-label clinical study in the third quarter of this year. The Phase 1 portion will assess the safety, tolerability, and preliminary clinical activity of AVZO-023 as a single agent and in combination therapy with endocrine therapy and with AVZO-021...in patients with advanced or metastatic hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer and select other advanced solid tumors."

IND • Licensing / partnership • New P1/2 trial • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

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