Kardorisso (asandeutertinib) / TYK Medicines - LARVOL DELTA

A phase II study of asandeutertinib (TY-9591) in advanced NSCLC patients with EGFR-positive mutations and brain metastases. (ASCO 2025) - P1, P2, P3 | "Asandeutertinib is highly effective and well-tolerated in locally advanced or metastatic EGFRm+ NSCLC patients with BM. Pivotal phase II study (NCT05948813) and phase II trials (NCT05382728) are onging. Keywords: TY-9591; Deuterated osimertinib derivative; Brain metastases."

Clinical • Metastases • P2 data • Cardiomyopathy • Cardiovascular • Interstitial Lung Disease • Keratitis • Lung Cancer • Non Small Cell Lung Cancer • Ocular Inflammation • Oncology • Ophthalmology • Pulmonary Disease • Respiratory Diseases • Solid Tumor • EGFR

Comparison of Asandeutertinib and Osimertinib in EGFR-Mutated NSCLC With Brain Metastases: Interim Analysis of the ESAONA Pivotal Study (IASLC-WCLC 2025) - "Conclusions : The interim results of ESAONA-pivotal study demonstrated that asandeutertinib pronouncedly improved intracranial efficacy compared to osimertinib with a manageable safety profile. Asandeutertinib is a promising new first-line option for EGFR-mutated NSCLC patients with BM."

Dental Disorders • Interstitial Lung Disease • Leukopenia • Lung Cancer • Neutropenia • Non Small Cell Lung Cancer • Pulmonary Disease • Respiratory Diseases • Solid Tumor • Stomatitis • EGFR

Safety, Pharmacokinetics, and Efficacy of TY-9591 (Deuterated Osimertinib Derivative) in Advanced EGFR-mutated Non-Small Cell Lung Cancer: A Phase 1 Dose-Escalation and Dose-Expansion Study. (PubMed, J Thorac Oncol) - "TY-9591 demonstrated a favorable safety profile and substantial efficacy in treating EGFR-mutated NSCLC, especially in patients with L858R mutations."

Journal • P1 data • PK/PD data • Hematological Disorders • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Efficacy and safety of asandeutertinib versus osimertinib as first-line treatment in EGFR-mutated NSCLC patients with brain metastases: Interim analysis of an open-label, multicenter, randomized, pivotal phase II study (ESAONA). (ASCO 2026) - P2 | "Asandeutertinib significantly improved iORR and iPFS compared to osimertinib, with manageable safety profile, supporting its potential as a new first-line treatment for EGFR-mutated NSCLC pts with BM."

Clinical • Late-breaking abstract • P2 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • EGFR

TYK Medicines…announced that its self-developed next-generation EGFR-TKI innovative drug, Deuterated Osemitinib Tablets (TY-9591 Tablets), has received conditional marketing approval from China’s National Medical Products Administration (NMPA). (BigGo) - "The approved indication is first-line treatment for adult patients with EGFR-mutant non-small cell lung cancer (NSCLC) with central nervous system metastases."

China approval • Non Small Cell Lung Cancer

ESAONA: TY-9591 in the Patients With EGFR Mutations in Advanced NSCLC With Brain Metastases (clinicaltrials.gov) - P2 | N=420 | Recruiting | Sponsor: TYK Medicines, Inc | Trial completion date: Dec 2027 ➔ Mar 2030 | Trial primary completion date: Jun 2025 ➔ Dec 2025

Trial completion date • Trial primary completion date • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

TYK Medicines’ Asandeutertinib Shows Superior Brain Metastasis Control in Phase II Lung Cancer Trial (TipRanks) - "The study, which enrolled 224 patients and had a median follow-up of just over 19 months, found that intracranial responses and durability of response with asandeutertinib had not yet reached median values, while the comparator arm had, suggesting a potential long-term control advantage. These data, presented as a late-breaking abstract at the 2026 American Society of Clinical Oncology annual meeting..."

Late-breaking abstract • P2 data • Non Small Cell Lung Cancer

The selective Yap/Tead inhibitor TY-1054 re-sensitizes acquired resistance to multiple tyrosine kinase-based targeted therapies (AACR 2025) - P1, P1/2 | "Small molecules that block auto-palmitoylation of TEADs, such as VT3989 (NCT04665206) and BPI-460372 (NCT05789602), have been successfully to enter the clinical trials. TY-1054 had excellent efficacy in the H226 CDX and HNSCC PDX mouse models. TY-9591 is a third-generation EGFR inhibitor developed by TYK Medicines and is currently under pivotal Phase III clinical investigation in China. Our studies showed that TY-9591 had excellent efficacy in the PC9 CDX mouse model, but tumors gradually recurred, as Osimertinib did."

Preclinical • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck

TYK Medicines Inc Announces Inclusion Of Asandeutertinib In List Of Products For Priority Review By Center For Drug Evaluation Of NMPA China (TradingView)

China filing • Priority review • Non Small Cell Lung Cancer

Tongyuan Kang Pharmaceutical-B...announced that its investigational Class 1 new drug, Edotinib Mesylate Tablets (TY-9591 tablets), has been proposed for inclusion in the priority review list by the Center for Drug Evaluation of the National Medical Products Administration. [Google translation] (Yahoo Finance) - "The proposed indication is: first-line treatment for adult patients with locally advanced or metastatic non-small cell lung cancer who have epidermal growth factor receptor exon 19 deletion or exon 21 substitution mutation, accompanied by central nervous system metastases."

EGFR exon 20 • Priority review • Non Small Cell Lung Cancer

TYK Medicines, Inc.’s EGFR-Targeted Innovative Drug Asandeutertinib Demonstrates Excellent Efficacy in NSCLC Patients with Brain Metastases — Interim Results from the ESAONA Pivotal Study Announced at WCLC 2025 (TYK Medicines Press Release) - "Based on interim analysis of 224 patients, BICR-assessed iORR of asandeutertinib was 91.9% (95% CI: 85.2–96.2) vs. 76.1% (95% CI: 67.2–83.6, P = 0.001) of osimertinib; investigator-assessed iORR of asandeutertinib was 91.0% (95% CI: 84.1–95.6) vs. 75.2% (95% CI: 66.2–82.9, P = 0.002) of osimertinib. Overall ORR favorable trended asandeutertinib with 84.7% comparing osimertinib with 75.2%. iPFS, PFS, OS, and other efficacy data were not yet mature."

P2 data • Non Small Cell Lung Cancer

Old Wine in New Bottles? Deuterium Switch (Replacing Hydrogen With Deuterium) Comes to Thoracic Oncology as Deuterated Lorlatinib (Deulorlatinib, TGRX-326) and Deuterated Osimertinib (Asandeutertinib, TY-9591) in ALK+ NSCLC and EGFR+ NSCLC, Respectively. (PubMed, J Thorac Oncol) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

JTO Published Phase I Study Results of Asandeutertinib Mesylate Tablets (TYK Medicines Press Release) - P1 | N=105 | NCT04204473 | Sponsor: TYK Medicines, Inc | "The published phase I study (NCT04204473) is a single-arm, open-label, dose-escalation and dose-expansion clinical trial evaluating the safety, pharmacokinetics, and efficacy of Asandeutertinib Mesylate Tablets in patients with advanced EGFR-mutant NSCLC....According to AUC0-t calculations, the exposure of the active metabolite D1 was 5.16%~7.09% of the parent drug across all dosage groups, while the exposure of the active metabolite D2 was 4.75%~13.2% of the parent drug....Based on FAS efficacy analysis, the median progression-free survival (PFS) was 21.5 months (95% CI: 17.3-27.3), and the OS data were not mature. Seven patients (8.9%) experienced disease progression due to brain metastases, with the lowest incidence of 8.3% observed in the 160 mg dose group (only one case, in a patient with pre-existing brain metastasis at baseline)."

P1 data • Non Small Cell Lung Cancer

INVESTIGATOR DATA SHOW PIVOTAL PHASE II CLINICAL TRIAL OF TY-9591 VERSUS OSIMERTINIB AS A FIRST-LINE TREATMENT FOR BRAIN METASTASES FROM LUNG CANCER WITH EGFR MUTATIONS MET EXPECTATIONS WITH STATISTICAL AND CLINICAL SIGNIFICANCE (HKEXnews) - P2 | N=420 | NCT05948813 | Sponsor: TYK Medicines, Inc | "The trial results show that: The iORR, as the primary study endpoint, met expectations and TY-9591 demonstrated notably improved statistical and clinical significance over osimertinib....Among 224 enrolled subjects in the trial, 53.1% had a deletion of exon 19 and 46.9% had a mutation in exon 21 L858R, in line with the distribution of mutation levels in real-world patients. The TY-9591 demonstrated an overall favorable safety profile, with no new safety signals observed. Detailed data from this clinical study will be presented at international or domestic clinical conferences in the near future. The Company plans to submit an NDA (New Drug Application) to the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) in the near future."

P2 data • Non Small Cell Lung Cancer

Studies Evaluating the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of TY-9591 Tablets in Healthy Subjects (clinicaltrials.gov) - P1 | N=48 | Completed | Sponsor: TYK Medicines, Inc | Recruiting ➔ Completed | Trial completion date: Aug 2024 ➔ Dec 2024

Trial completion • Trial completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

[14 C] Study on Mass Balance of TY-9591 in Healthy Chinese Subjects (clinicaltrials.gov) - P1 | N=6 | Completed | Sponsor: TYK Medicines, Inc | Recruiting ➔ Completed | N=10 ➔ 6

Enrollment change • Trial completion

Study of TY-9591 in Patients With a Lung Cancer With Brain or Leptomeningeal Metastases With EGFR Mutation (clinicaltrials.gov) - P2 | N=29 | Completed | Sponsor: TYK Medicines, Inc | Active, not recruiting ➔ Completed | N=60 ➔ 29

Enrollment change • Trial completion • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TY-9591 With Chemotherapy as 1st Line Treatment in Patients With Mutated Epidermal Growth Factor Receptor NSCLC (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: TYK Medicines, Inc

Metastases • New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Phase 1 Study of TY-9591 in Advanced Non-Small Cell Lung Cancer (NSCLC) Patients with EGFR Positive Mutation. (IASLC-WCLC 2024) - P1, P2, P3 | "Conclusions : TY-9591 is a highly effective and well-tolerated third-generation EGFR TKI for patients with EGFR sensitizing mutation advanced NSCLC, especially for patients with L858R mutations or with brain metastases. Pivotal phase 2 (NCT05948813) and phase 3 trials (NCT05382728) are onging."

Clinical • Metastases • P1 data • Anemia • Cardiomyopathy • Cardiovascular • Hematological Disorders • Interstitial Lung Disease • Keratitis • Lung Cancer • Non Small Cell Lung Cancer • Ocular Inflammation • Oncology • Ophthalmology • Pulmonary Disease • Respiratory Diseases • Solid Tumor • EGFR

The Results of Asandeutertinib Tablets (TY-9591) will be Presented at the WCLC 2024 (TYK Medicines Press Release) - P1a/b | N=105 | NCT04204473 | Sponsor: TYK Medicines, Inc | "The phase Ⅰ study results of the innovative drug asandeutertinib tablets (TY-9591) developed by TYK medicines to treat advanced EGFR mutation-positive NSCLC will be presented at this conference....The median PFS of TY-9591 as a first-line treatment for EGFR-sensitive mutation (19del or L858R) NSCLC patients was 21.5 months, with 25.7 months in the 19del subgroup and 19.3 months in the L858R subgroup.The confirmed ORR was 85.9%, DCR was 96.2%, tumor response depth (DepOR) was 50.46%, and the median DoR was 20.2 months....The exposure (AUC) of the toxic metabolite TY-9591-D1 was about 4.76-6.36% of the parent drug under steady state."

P1 data • PK/PD data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TYK Medicines raises $74M IPO to fund EGFR cancer therapy (Firstwordpharma Press Release) - "TYK Medicines has raised about $74.3 million (HKD 579 million) through an IPO, with plans to allocate a portion to advance its core asset TY-9591....Additionally, TYK has been given the okay in China for Phase II and Phase III trials of TY-9591 in combination with chemotherapy for advanced or metastatic EGFR-mutated NSCLC, with plans to initiate Phase II testing in the second half....TY-302, a CDK4/6 inhibitor, is considered a key asset in Phase II development for second-line breast cancer in China, with plans to enter a registrational trial early next year. The biotech also has another Phase II trial planned for TY-302 in first-line prostate cancer, set to begin in the second half of 2024."

Financing • New P2 trial • New trial • Genito-urinary Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor

Tongyuankang Pharmaceuticals went public in Hong Kong with a valuation of over 3 billion (Sina Corp) - "The company is currently conducting a pivotal Phase II clinical trial of TY-9591 monotherapy in China for the first-line treatment of brain metastases in non-small cell lung cancer ('NSCLC') with epidermal growth factor receptor ('EGFR') mutations, and expects to submit an NDA in Q1 2025. The company expects to be approved for marketing in China in the fourth quarter of 2025. A registrational Phase III clinical trial of TY-9591 monotherapy is currently underway in China for the first-line treatment of locally advanced (stage IIIb or IV) or metastatic NSCLC with EGFR L858R mutation, and an NDA submission is expected in the second half of 2026."

China approval • China filing • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Studies Evaluating the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of TY-9591 Tablets in Healthy Subjects (clinicaltrials.gov) - P1 | N=48 | Recruiting | Sponsor: TYK Medicines, Inc

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Study of TY-9591 in Patients With a Lung Cancer With Brain or Leptomeningeal Metastases With EGFR Mutation (clinicaltrials.gov) - P2 | N=60 | Active, not recruiting | Sponsor: TYK Medicines, Inc | Recruiting ➔ Active, not recruiting

Enrollment closed • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TY-9591 in Advanced Non-small Cell Lung Cancer(NSCLC) Patients With EGFR Positive Mutation (clinicaltrials.gov) - P1 | N=105 | Completed | Sponsor: TYK Medicines, Inc | Recruiting ➔ Completed

Metastases • Trial completion • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor