sudocetaxel zendusortide (TH 1902) / Theratechnologies - LARVOL DELTA

Efficacy and safety data from Ph1b, dose optimization trial of two doses of TH1902 (sudocetaxel zendusortide), a novel SORT1-targeting peptide drug conjugate (PDC), administered weekly vs q3weekly in patients (pts) with advanced ovarian cancer. (ASCO 2025) - P1 | "Via SORT1 receptor's normal trafficking function, rapid internalization and release of the docetaxel payload is achieved, resulting in higher intracellular concentrations compared to docetaxel alone. Weekly administration of TH1902 resulted in an improved safety profile, with no DLTs, few ≥Gr 3 TRAEs, and no ≥Gr 3 neuropathy, ocular or neutropenia events. An emerging efficacy signal in the higher dose arm suggests a dose response. Two additional monotherapy doses will be explored in the proposed amendment (i.e."

Clinical • Metastases • Endometrial Cancer • Neutropenia • Oncology • Optic Neuritis • Ovarian Cancer • Pain • Solid Tumor • MUC16

TH1902-CTR-0001: TH1902 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=70 | Active, not recruiting | Sponsor: Theratechnologies | Trial completion date: Dec 2024 ➔ Jan 2026 | Trial primary completion date: Dec 2024 ➔ Dec 2025 | Recruiting ➔ Active, not recruiting

Enrollment closed • Trial completion date • Trial primary completion date • Breast Cancer • Cholangiocarcinoma • Cutaneous Melanoma • Endocrine Cancer • Endometrial Cancer • Epithelial Ovarian Cancer • Genito-urinary Cancer • Hepatocellular Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Melanoma • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Prostate Cancer • Skin Cancer • Small Cell Lung Cancer • Solid Tumor • Thyroid Gland Carcinoma • Triple Negative Breast Cancer • CD4

Theratechnologies Reports Financial Results for the Fourth Quarter and Full Year of Fiscal 2024 (GlobeNewswire) - "Sudocetaxel Zendusortide (TH1902) and SORT1+ Technology:...On January 31, 2025, the Company received FDA approval to proceed with an amendment to its Phase 1 study protocol to increase the dose of sudocetaxel zendusortide on the same weekly infusion cycle to 3.33 followed by 3.90 mg/kg/wk. The Company is currently reaching out to pharmaceuticals companies to out-license the rights to sudocetaxel zendusortide and to its SORT1+ Technology platform."

Clinical protocol • Commercial • FDA event • Ovarian Cancer

Theratechnologies Announces Preliminary Tolerability and Efficacy Data from Phase 1b, Dose-Ranging Trial of Sudocetaxel Zendusortide in Patients with Advanced Ovarian Cancer (GlobeNewswire) - P1 | N=70 | NCT04706962 | Sponsor: Theratechnologies | "A total of 13 patients with advanced ovarian cancer who progressed despite prior platinum-based and taxane chemotherapy were enrolled in two Arms in Part 3 of the Phase 1b trial...Investigators observed no dose-limiting toxicities in either arm. Although there were no responses observed in the five Arm A participants that comprised the per-protocol (PP) set, there was encouraging evidence of activity observed in three of the six patients enrolled in the Arm B PP set, including one patient with a complete resolution of a liver lesion. Those three Arm B patients also experienced significant reductions in the CA-125 ovarian tumor marker as well as significant tumor shrinkage, including two patients with more than a 25% reduction in tumor size. In addition....there is also an extensive body of preclinical data demonstrating the flexibility of the Company’s SORT1+ Technology platform when conjugated with different toxic payloads."

P1 data • Preclinical • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Long-term efficacy, safety and PK data of TH1902 (sudocetaxel zendusortide) in solid tumors: A novel SORT1-targeting peptide-drug-conjugate (PDC). (ASCO 2024) - P1 | "TH1902 induces durable disease stabilization that lasts beyond treatment completion, suggesting a unique, multimodal mechanism of action (MOA) that differs from other cancer therapeutics. TH1902 has a manageable safety profile at 300mg/m 2 with few Gr3 AEs. Low levels of free docetaxel in human plasma may in part explain the low rate of taxane related AEs (i.e."

Clinical • PK/PD data • Alopecia • Anemia • Endometrial Cancer • Hematological Disorders • Immunology • Keratitis • Melanoma • Neutropenia • Ocular Inflammation • Oncology • Ophthalmology • Pain • Solid Tumor • Triple Negative Breast Cancer

Theratechnologies’ Sudocetaxel Zendusortide ASCO 2024 Presentation Demonstrates Signs of Long-Term Efficacy and Manageable Safety Profile in Patients with Solid Tumors (GlobeNewswire) - P1 | N=70 | NCT04706962 | Sponsor: Theratechnologies | "Theratechnologies Inc....announced Phase 1 data demonstrating signs of long-term efficacy and a manageable safety profile of its lead investigational peptide drug conjugate (PDC) candidate, sudocetaxel zendusortide (TH1902), in patients with solid tumors. The data will be presented...at the 2024 American Society of Clinical Oncology (ASCO)...In an updated analysis from Parts 1 and 2 of an ongoing Phase 1 clinical trial, sudocetaxel zendusortide induced durable disease stabilization (up to 45 weeks) lasting beyond treatment completion...Additionally, investigators observed an early efficacy signal primarily in female cancers (ovarian cancer, endometrial cancer, triple-negative breast cancer [TNBC]), with seven of 16 participants (44%) achieving a clinical benefit rate (complete response + partial response + stable disease)....PK measures showed that exposure to free docetaxel was much lower than that for sudocetaxel..."

P1 data • PK/PD data • Endometrial Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor • Triple Negative Breast Cancer

Theratechnologies to Present Long-Term Efficacy, Safety and Pharmacokinetic Data on Use of TH1902 (sudocetaxel zendusortide) in Solid Tumors at 2024 ASCO Meeting (GlobeNewswire) - "Theratechnologies...announced that it will present long-term efficacy, safety and pharmacokinetic (PK) data on the use of its lead investigational peptide-drug conjugate (PDC) candidate, TH1902 (sudocetaxel zendusortide), in patients with solid tumors....The ASCO poster represents the first presentation of long-term data from Part 1 (dose escalation) and Part 2 (dose expansion) of Theratechnologies’ Phase 1 clinical trial of sudocetaxel zendusortide in individuals with solid tumors....This updated analysis will present further data on long-term efficacy, safety and PK from Parts 1 and 2, focusing specifically on patients receiving sudocetaxel zendusortide at a dose of 300 mg/m2 every three weeks. Patients in this dosing group have cancers with known high expression of sortilin (SORT1), including ovarian cancer, endometrial cancer, triple-negative breast cancer (TNBC) and melanoma."

P1 data • PK/PD data • Endometrial Cancer • Melanoma • Ovarian Cancer • Triple Negative Breast Cancer

Sudocetaxel Zendusortide (TH1902) triggers the cGAS/STING pathway and potentiates anti-PD-L1 immune-mediated tumor cell killing (AACR 2024) - "Surprisingly, immunohistochemistry analysis revealed higher staining of CD45 leukocytes and of STING, a master regulator in the cancer-immunity cycle, in comparison to docetaxel. Accordingly, TH1902 inhibited cell proliferation and triggered apoptosis and senescence in B16-F10 cells in vitro, while inducing several downstream effectors of the cGAS/STING pathway and the cell surface expression of MHC-I and PD-L1. This is the first evidence that TH1902 exerts its antitumor activity, in part, through modulation of the iTME and that the combination of TH1902 with checkpoint inhibitors (anti-PD-L1) could lead to improved clinical outcomes."

IO biomarker • Tumor cell • Breast Cancer • Melanoma • Oncology • Solid Tumor • Triple Negative Breast Cancer • CASP3 • GZMB • PTPRC • SORT1

Theratechnologies Preclinical Data Presentation at AACR 2024 Highlights Versatility and Flexibility of SORT1+ Technology Oncology Platform (GlobeNewswire) - "The investigators also described the preclinical effects of three PDCs – TH2101, TH2205, and TH2310 – that have a cytotoxic payload of SN-38, the active metabolite of irinotecan....In two different CRC xenograft models, as well as in the TNBC xenograft model, TH2303 was associated with increased tumor growth inhibition and greater tolerability compared to unconjugated exatecan or irinotecan....In another experiment described in the poster, the combination of two SORT1-targeting PDCs - sudocetaxel zendusortide (TH1902) and TH2101, which have a synergistic anti-tumor effect at reduced doses, led to increased tumor growth inhibition and some complete responses in the HT-29 xenograft model, compared to either PDC administered alone."

Preclinical • Colorectal Cancer • Triple Negative Breast Cancer

Theratechnologies to Present Preclinical Data at AACR on Multiple PDCs Showcasing Potential of SORT1+Technology Platform (GlobeNewswire) - "These preclinical presentations reinforce existing data for sudocetaxel zendusortide to activate anti-PD-L1 immunotherapy tumor cell killing in SORT+1 cancers and provide the first evidence for novel camptothecin-peptide conjugates in the treatment of SORT+1 colorectal cancers."

Preclinical • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Theratechnologies Announces Update on its Preclinical Oncology Research Program (GlobeNewswire) - "Theratechnologies Inc...today announced that it will phase down its preclinical oncology research activities. The Company will continue to prioritize its ongoing Phase 1 clinical trial of sudocetaxel zendusortide (TH1902), a novel peptide-drug conjugate (PDC), in patients with advanced ovarian cancer...The Company will continue to share accumulated preclinical data, including the presentation of two separate posters at the American Association for Cancer Research (AACR) annual meeting, to be held April 5-9 in San Diego, Calif., one of which features data from new PDCs....Recruitment has been ramped up at the six trial sites across North America. To date, more than 40 individuals with various types of cancer have been treated with sudocetaxel zendusortide."

Preclinical • Trial status • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Theratechnologies Initiates Increased Dose Level in Phase 1 Clinical Trial of Sudocetaxel Zendusortide in Advanced Ovarian Cancer (GlobeNewswire) - "Theratechnologies Inc...today announced moving to the next dose level in Part 3 of its Phase 1 clinical trial of sudocetaxel zendusortide in patients with advanced ovarian cancer. The study’s Medical Review Committee (MRC) has deemed the dose level in the first cohort of patients safe and has approved initiation of the next cohort with an increased dose, in accordance with the updated dose optimization protocol. Study centers are now actively recruiting patients for the second cohort, with one patient already enrolled and treated with the higher dose."

Trial status • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Sudocetaxel Zendusortide (TH1902) triggers the cGAS/STING pathway and potentiates anti-PD-L1 immune-mediated tumor cell killing. (PubMed, Front Immunol) - "A weekly administration of TH1902 as a single agent in a murine B16-F10 melanoma syngeneic tumor model demonstrated superior tumor growth inhibition than did docetaxel. TH1902 inhibited cell proliferation and triggered apoptosis and senescence in B16-F10 cells in vitro, while inducing several downstream effectors of the cGAS/STING pathway and the expression of MHC-I and PD-L1. This is the first evidence that TH1902 exerts its antitumor activity, in part, through modulation of the immune tumor microenvironment and that the combination of TH1902 with checkpoint inhibitors (anti-PD-L1) could lead to improved clinical outcomes."

IO biomarker • Journal • Tumor cell • Breast Cancer • Melanoma • Oncology • Solid Tumor • Triple Negative Breast Cancer • CASP3 • GZMB • PTPRC • SORT1

Theratechnologies Announces Publication in Frontiers in Immunology that Deepens Understanding of Sudocetaxel Zendusortide (TH1902) Molecular Mechanism of Action (GlobeNewswire) - "Theratechnologies Inc...today announced the publication of a peer-reviewed article in Frontiers in Immunology that enhances understanding of the molecular mechanism of action of sudocetaxel zendusortide (also known as TH1902) as a potential anticancer treatment....It reports on preclinical research in which sudocetaxel zendusortide induced complete and prolonged tumor regression in a triple-negative breast cancer (TNBC)-derived xenograft tumor model and demonstrated tumor regression associated with growth inhibition and immune cell infiltration in a 'cold' murine (syngeneic) tumor model. Additionally, combining sudocetaxel zendusortide with an anti-PD-L1 checkpoint inhibitor led to increases in tumor growth inhibition and median animal survival."

Preclinical • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Theratechnologies Completes Enrollment of First Six Patients in Updated Phase 1 Clinical Trial of Sudocetaxel Zendusortide in Advanced Ovarian Cancer (GlobeNewswire) - "Theratechnologies Inc...today announced completion of enrollment of the first six participants in Part 3 of its Phase 1 clinical trial of sudocetaxel zendusortide in patients with advanced ovarian cancer. Sudocetaxel zendusortide, also known as TH1902, is an investigational, first-in-class peptide-drug conjugate (PDC) that targets the sortilin receptor (SORT1) and aims to expedite the internalization and delivery of the cytotoxic payload (docetaxel) directly into cancer cells...After establishing the safety of the initial dose in the first six patients for a period of three months, the enrollment of the next cohort of six patients at a higher dose will be initiated."

Enrollment status • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Theratechnologies Receives 2023 CQDM ADRIQ RSRI Innovation Award (GlobeNewswire) - "Theratechnologies Inc...today announced receipt of the 2023 Industrial Research Sectoral Group (RSRI) Innovation Award from the CQDM (formerly known as the Québec Consortium for Drug Discovery) and the Association for the Development of Research and Innovation of Québec (ADRIQ). The award recognizes the company’s work, in partnership with world-renowned cancer researcher Professor Borhane Annabi of the Université du Québec à Montréal (UQAM), in demonstrating the preclinical efficacy of its investigational peptide-drug conjugate TH1902 (sudocetaxel zendusortide) against triple-negative breast cancer....A Phase 1 clinical trial is currently underway with five study sites simultaneously enrolling patients in the U.S., as well as a Canadian site set to begin recruitment at the Centre Hospitalier de l'Université de Montréal."

Enrollment status • Preclinical • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Theratechnologies Announces Operational Update (GlobeNewswire) - "Theratechnologies Inc...announced further changes to its operations that will see a tapering of R&D activities, which necessitates a reduction of up to 25 positions. The Company expects to realize recurring yearly savings of approximately US$3.5 million resulting from this reorganization and will record a restructuring charge of approximately US$1.5 million in its fourth quarter of 2023....The Company is committed to delivering on Part 3 of the Phase 1 clinical trial in advanced ovarian cancer for sudocetaxel zendusortide. All future clinical research activities in oncology and NASH will be made through partnership deals."

Commercial • P1 data • Gynecologic Cancers • Oncology • Ovarian Cancer

Sudoxetaxel zendusortide (TH1902): A Novel Peptide Drug Conjugate's Journey From the Preclinical to the Clinical Setting (ADC-USA 2023) - "Understanding the potential utility of Sortilin as a biomarker for cancer; Introducing Sudocetaxel zendusortide as a promising therapy for metastatic cancer with a unique mechanism of action that involves rapid internalization into cancer cells through the Sortilin receptor; Reviewing the ongoing Phase I FIH study investigating Sudocetaxel zendusortide, including its study design, dosing, safety, and early signs of efficacy"

Preclinical • Oncology • SORT1

Theratechnologies Announces Dosing of First Patient in Updated Clinical Trial of Sudocetaxel Zendusortide in Advanced Ovarian Cancer (GlobeNewswire) - "Theratechnologies Inc...today announced dosing of the first participant in Part 3 of its Phase 1 clinical trial of sudocetaxel zendusortide in patients with advanced ovarian cancer....Enrollment of the first patient in Part 3 of the trial follows closely upon demonstration of antitumor activity in Parts 1 and 2, as presented at the 2023 annual meeting of the American Society of Clinical Oncology."

Trial status • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Theratechnologies Announces All U.S. Oncology Clinical Sites Now Enrolling for Phase 1 Trial of Sudocetaxel Zendusortide (GlobeNewswire) - "Theratechnologies...announced that all five of the U.S.-based clinical sites participating in the conduct of the Phase 1 clinical trial of the Company’s lead investigational peptide drug conjugate, sudocetaxel zendusortide, are now activated to screen, enroll and dose advanced ovarian cancer patients. A sixth site based in Canada is finalizing its start-up activity."

Trial status • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

TH1902 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=70 | Recruiting | Sponsor: Theratechnologies | Active, not recruiting ➔ Recruiting

Enrollment open • Metastases • Breast Cancer • Cholangiocarcinoma • Cutaneous Melanoma • Endocrine Cancer • Endometrial Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatocellular Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Melanoma • Neuroendocrine Tumor • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Prostate Cancer • Skin Cancer • Small Cell Lung Cancer • Solid Tumor • Thyroid Gland Carcinoma • Triple Negative Breast Cancer • CD4

TH1902 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=70 | Active, not recruiting | Sponsor: Theratechnologies | Trial completion date: Mar 2023 ➔ Dec 2024 | Trial primary completion date: Mar 2023 ➔ Dec 2024

Metastases • Trial completion date • Trial primary completion date • Breast Cancer • Cholangiocarcinoma • Cutaneous Melanoma • Endocrine Cancer • Endometrial Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatocellular Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Melanoma • Neuroendocrine Tumor • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Prostate Cancer • Skin Cancer • Small Cell Lung Cancer • Solid Tumor • Thyroid Gland Carcinoma • Triple Negative Breast Cancer • CD4

Theratechnologies June 13 Oncology Investigator Call to Update Investors & Analysts on Phase 1 Sudocetaxel Zendusortide Trial (GlobeNewswire) - "Theratechnologies Inc...will hold a video conference call on Tuesday, June 13, 2023, to update investors and analysts on the Phase 1 trial of its lead peptide-drug conjugate (PDC) candidate, sudocetaxel zendusortide (formerly TH1902), for the treatment of solid tumors. During the call, Theratechnologies will provide insights on preliminary Phase 1 safety and efficacy data that were presented at the 2023 annual meeting of the American Society of Clinical Oncology (ASCO), as well as the U.S. Food and Drug Administration’s (FDA) recent agreement to the Company’s amended Phase 1 trial protocol."

Clinical protocol • P1 data • Breast Cancer • Cutaneous Melanoma • Endocrine Cancer • Endometrial Cancer • Genito-urinary Cancer • Gynecologic Cancers • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Melanoma • Oncology • Ovarian Cancer • Prostate Cancer • Skin Cancer • Small Cell Lung Cancer • Solid Tumor • Thyroid Gland Carcinoma • Triple Negative Breast Cancer

Sudocetaxel zendusortide (TH1902), a novel sortilin-receptor (SORT1)-targeting peptide-drug-conjugate (PDC) in patients (pts) with advanced solid tumors: Results from part 1 (dose-escalation) of a phase 1, open-label study. (ASCO 2023) - P1 | "TH1902 is a first-in-class PDC targeting SORT1, that consists of 2 molecules of docetaxel attached to the TH19P01 peptide via a cleavable succinyl linker. Although biological activity has been observed, the optimal dosing regimen of TH1902 is currently under evaluation. Clinical trial information: NCT04706962."

Clinical • Metastases • P1 data • Anemia • Hematological Disorders • Keratitis • Lung Cancer • Melanoma • Musculoskeletal Pain • Neutropenia • Non Small Cell Lung Cancer • Ocular Inflammation • Oncology • Ophthalmology • Pain • Solid Tumor • ER • HER-2 • SORT1

Theratechnologies Receives FDA Agreement to Amended Trial Protocol for its Lead PDC Candidate Sudocetaxel Zendusortide (GlobeNewswire) - "Theratechnologies Inc...announced that the U.S. Food and Drug Administration (FDA) has agreed to the Company’s amended protocol for the Phase 1 clinical trial of sudocetaxel zendusortide, an investigational, first-in-class peptide-drug conjugate (PDC) that targets the sortilin (SORT1) receptor and expedites the internalization and delivery of a cytotoxic payload directly into cancer cells. Today’s announcement also marks the lifting of the FDA’s partial clinical hold on the Phase 1 trial, following the Company’s voluntary pause of patient recruitment in December 2022."

FDA event • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor