EIK1001 / Seven and Eight BioPharma, Eikon Therap - LARVOL DELTA

Safety and efficacy of EIK1003, a selective PARP1 inhibitor, as monotherapy in participants with advanced solid tumors. (ASCO 2025) - "Funded by No funding sources reported Clinical Trial Registration Number: 06253130 Background: PARP inhibitors (PARPi) selectively kill tumor cells with genetic mutations in critical DNA repair genes (eg, BRCA1/2). To date, EIK1001 has demonstrated tolerable safety and encouraging preliminary efficacy. Dose escalation is ongoing. Updated safety and efficacy data will be reported at the time of presentation."

Clinical • Metastases • Monotherapy • Anemia • Breast Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Neutropenia • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor • BRCA1 • BRCA2 • HER-2 • HRD • MUC16 • PARP2

TeLuRide-006: An adaptive phase 2/3 study of EIK1001, a Toll-like receptor 7/8 (TLR7/8) agonist, in combination with pembrolizumab in patients with advanced melanoma. (ASCO 2025) - "Exploratory objectives include evaluation of time to objective response, evaluation of potential EIK1001 exposure-response relationships, and evaluation of health-related quality of life, health utilities, and melanoma concerns in pts receiving EIK1001 + pembro relative to placebo + pembro. This study opened on 24 December 2024."

Clinical • Combination therapy • IO biomarker • Metastases • P2/3 data • Interstitial Lung Disease • Melanoma • Oncology • Pneumonia • Pulmonary Disease • Respiratory Diseases • Solid Tumor • BRAF

Recent Program Milestones (Businesswire) - "(i) EIK1001-006 (TeLuRide-006, NCT06697301): The first patient has been enrolled in the TeLuRide-006 trial, which is investigating the potential role of EIK1001, a systemically administered co-agonist of toll-like receptors 7 and 8 that has been observed to exhibit clinical activity as a monotherapy and in combination with anti-PD-(L)1 agents across multiple solid tumor types in Phase 1 trials, as an addition to standard of care pembrolizumab (KEYTRUDA) for the treatment of patients with advanced metastatic melanoma...; (ii) EIK1004-001 (NCT06907043): The first patient has been dosed in a Phase 1/2 trial of EIK1004, a CNS-penetrant selective PARP1 inhibitor."

Trial status • Melanoma

Eikon Therapeutics to Share Clinical Data and Program Updates at the 2025 ASCO Annual Meeting (Businesswire) - "Eikon Therapeutics...announced that new data from its oncology programs will be presented in collaboration with independent investigators at the American Society of Clinical Oncology (ASCO) Annual Meeting....The...posters will spotlight new first-in-human and combination data from Eikon’s two most advanced clinical programs."

Clinical protocol • P1/2 data • Melanoma

Immunity induction with atezolizumab, EIK1001, and radiotherapy in virus-associated tumors: Results of the AGADIR Trial (AACR 2025) - "The combination of atezolizumab, EIK1001, and radiotherapy met its primary endpoint of disease control rate at 24 weeks, underscoring the potential of this regimen. in virus-associated tumors, particularly HPV-related cancers. Biomarker analyses support the immunogenic potential of this regimen, suggesting a paradigm shift in treating immunologically 'cold' virus-associated tumors."

IO biomarker • Cervical Cancer • Head and Neck Cancer • Oncology • Oropharyngeal Cancer • Solid Tumor

KEYNOTE-914: BDB001-101: Clinical Study of BDB001 as a Mono-therapy or in Combination With Pembrolizumab (clinicaltrials.gov) - P1 | N=87 | Completed | Sponsor: Eikon Therapeutics | Active, not recruiting ➔ Completed | N=50 ➔ 87 | Trial completion date: Aug 2024 ➔ Apr 2024 | Trial primary completion date: Aug 2024 ➔ Mar 2024

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

BDB001-102: Open Label Dose Escalation of BDB001 in Combination w Atezolizumab (clinicaltrials.gov) - P1 | N=40 | Completed | Sponsor: Eikon Therapeutics | Active, not recruiting ➔ Completed

Trial completion • Oncology • Solid Tumor • CTLA4 • IL2 • TNFRSF9

KEYNOTE-G04: Safety and Efficacy of EIK1001-006 in Combo With Pembro Versus Placebo and Pembro as First-Line Therapy in Patients With Advanced Melanoma. (clinicaltrials.gov) - P2/3 | N=740 | Recruiting | Sponsor: Eikon Therapeutics | Initiation date: Nov 2024 ➔ Apr 2025 | Not yet recruiting ➔ Recruiting

Enrollment open • Trial initiation date • Melanoma • Oncology • Solid Tumor

Eikon Therapeutics Secures $350.7 Million Series D to Advance Clinical-Stage Programs and Future Pipeline (Businesswire) - "Eikon Therapeutics, Inc...announced the initial closing of a $350.7 million Series D financing. Since its founding in 2019, Eikon Therapeutics has privately raised in excess of $1.1 billion to support its mission of developing new medicines to address grievous illnesses....Eikon’s clinical portfolio is anchored by its lead program, EIK1001, a systemically administered co-agonist of toll-like receptors 7 and 8 now in a Phase III trial for advanced melanoma.... In parallel, the company is advancing EIK1003, a highly selective PARP1 inhibitor currently undergoing Phase 1 evaluation in patients with breast, ovarian, prostate, or pancreatic cancers, and EIK1004, a central nervous system-penetrant PARP1-selective inhibitor poised to initiate Phase 1 studies targeting brain cancers. Eikon’s early-stage pipeline features, among other undisclosed candidates, two androgen receptor antagonists and an internally derived WRN inhibitor (EIK1005)..."

Financing • Brain Cancer • Breast Cancer • Melanoma • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer

Examination of the potential clinical application of 5DEX-0509R, the tumor macrophage-targeting nanomedicine. (PubMed, Cytokine) - "To solve this, we have developed dextran-based TAM targeting activator conjugate (D-TAC) technology which successfully uses tumor-associated macrophages (TAMs) to deliver the TLR7 agonist DSP-0509...In this study, we compared the anti-tumor effects of EIK1001 and 5DEX-0509R, and analyzed its unique immune reaction against tumors to evaluate whether 5DEX-0509R is suitable for further clinical study...We also found that 5DEX-0509R synergistically suppresses tumors with oxaliplatin by changing M2 macrophages that cause oxaliplatin to become resistant to antitumor M1 macrophages. In addition, 5DEX-0509R caused a rapid but not sustained cytokine elevation in both rats and dogs. We believe 5DEX-0509R is worth pursuing for clinical trials."

Journal • Infectious Disease • Oncology • CD4

KEYNOTE-G04: Safety and Efficacy of EIK1001-006 in Combo With Pembro Versus Placebo and Pembro as First-Line Therapy in Patients With Advanced Melanoma. (clinicaltrials.gov) - P2/3 | N=740 | Not yet recruiting | Sponsor: Eikon Therapeutics

Combination therapy • Metastases • New P2/3 trial • Melanoma • Oncology • Solid Tumor

Effect of systemic TLR7/8 agonism on circulating immune cells in patients with advanced solid tumors (SITC 2024) - P1 | "Trial Registration Patient samples were acquired during the conduct of studies BDB001-101 (NCT03486301) and BDB001-102 (NCT04196530)...Ethics Approval For both clinical studies covered by this abstract, the Principal Investigator at each site was responsible for obtaining regional Ethics Committee (EC) or Institutional Review Board (IRB) approval for the final protocol, the Sponsor approved Informed Consent Form (ICF)/assent, participant information sheet, if applicable, and any advertisements to recruit participants. All patients provided informed consent prior to taking part in each study."

Clinical • Immune cell • IO biomarker • Metastases • Oncology • Solid Tumor • CXCL8 • IFNA1 • IFNG • IL6 • TLR7 • TLR8 • TNFA

Safety and preliminary efficacy of EIK1001 in combination with atezolizumab in participants with advanced solid tumors. (ASCO 2024) - P1 | "Overall, EIK1001 was well-tolerated with a manageable safety profile and showed encouraging preliminary efficacy across several tumor types in combination with atezolizumab. Responses were observed even in pts not anticipated to respond to atezolizumab monotherapy. Further development of EIK1001 is underway."

Clinical • Combination therapy • Metastases • Cardiovascular • Fatigue • Heart Failure • Oncology • Solid Tumor • PD-L1

A phase 2 study of EIK1001, a Toll-like receptor 7/8 (TLR7/8) agonist, in combination with pembrolizumab and chemotherapy in patients with stage 4 non-small cell lung cancer. (ASCO 2024) - P2 | " Study EIK1001-005 is a multicenter, Phase 2, open-label study of EIK1001 in combination with pembrolizumab and chemotherapy – carboplatin plus either pemetrexed or paclitaxel – in participants (pts) with histologically confirmed Stage 4 nonsquamous or squamous NSCLC, respectively. Other exploratory objectives include evaluation of anti-tumor activity (ORR/DOR) by immune-related RECIST 1.1, overall survival, progression-free survival, investigation of the relationship between treatment with EIK1001 in combination with pembrolizumab/chemotherapy and biomarkers predictive of response, and the pharmacokinetic parameters of EIK1001. This study opened on 29 Jan 2024."

Clinical • Combination therapy • IO biomarker • Metastases • P2 data • Lung Cancer • Lung Non-Small Cell Squamous Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Safety and preliminary efficacy of EIK1001 in combination with pembrolizumab in participants with advanced solid tumors. (ASCO 2024) - P1 | "Overall, EIK1001 was well-tolerated with a manageable safety profile and showed encouraging preliminary efficacy across several tumor types in combination with pembrolizumab. Responses were observed even in heavily pretreated patients not anticipated to respond to pembrolizumab monotherapy. Further development of EIK1001 is underway."

Clinical • Combination therapy • IO biomarker • Metastases • Cardiovascular • Dental Disorders • Fatigue • Hypertension • Oncology • Pancreatitis • Solid Tumor • Stomatitis • PD-L1

Sixteen Researchers from Florida Cancer Specialists & Research Institute Share Cancer Care Discoveries at 2024 ASCO Annual Meeting (PRNewswire) - "Florida Cancer Specialists & Research Institute, LLC (FCS) physicians will present findings from multiple clinical studies that are contributing to global advancements in cancer care at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting in Chicago. Clinical research originating from trials conducted at the three FCS Phase 1 Drug Development Units and late-phase studies at FCS clinics throughout Florida are among those being published or presented during the five-day international gathering of oncology physicians and professionals."

Clinical data • P1 data • P1/2 data • Breast Cancer • Liver Cancer • Non Small Cell Lung Cancer • Solid Tumor

Eikon Therapeutics Announces Multiple Abstracts to be Presented at the American Society of Clinical Oncology (ASCO) Annual Meeting (Businesswire) - "Separate poster presentations will highlight EIK1001 both in combination with pembrolizumab and chemotherapy (trial in progress) and safety and preliminary efficacy in combination with atezolizumab; A Phase 1 study of the PARP1-selective inhibitor, EIK1003, will be highlighted in a poster presentation (trial in progress)."

P1 data • Trial status • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Eikon Therapeutics Announces Multiple Abstracts to be Presented at the American Society of Clinical Oncology (ASCO) Annual Meeting (Businesswire) - P1 | N=50 | BDB001-101 (NCT03486301) | Sponsor: Eikon Therapeutics | "The oral presentation (Abstract: 2521) highlights safety and preliminary efficacy data from a clinical study (NCT03486301) of EIK1001, a Toll-like receptor 7/8 (TLR7/8) co-agonist, in combination with pembrolizumab in participants with advanced solid tumors. The new data show that EIK1001 was well-tolerated with a manageable safety profile, and showed encouraging preliminary efficacy across several tumor types in combination with pembrolizumab. Responses were observed even in heavily pretreated patients not anticipated to respond to pembrolizumab monotherapy."

P1 data • Oncology • Solid Tumor

BDB001-101: Clinical Study of BDB001 as a Mono-therapy or in Combination With Pembrolizumab (clinicaltrials.gov) - P1 | N=50 | Active, not recruiting | Sponsor: Eikon Therapeutics | Trial primary completion date: Mar 2024 ➔ Aug 2024 | Trial completion date: Mar 2024 ➔ Aug 2024

Combination therapy • Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

BDB001-102: Open Label Dose Escalation of BDB001 in Combination w Atezolizumab (clinicaltrials.gov) - P1 | N=40 | Active, not recruiting | Sponsor: Eikon Therapeutics | Trial completion date: Mar 2024 ➔ Jul 2024 | Trial primary completion date: Mar 2024 ➔ Jul 2024

Combination therapy • Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor • CTLA4 • IL2 • TNFRSF9

Pharmacokinetic/biomarker (PK/BMx) analysis of the toll-like receptor 7 and 8 (TLR7/8) agonist EIK1001 in phase 1 studies in participants (Pts) with solid tumors (AACR 2024) - P1 | "This dual activity provides another pathway, distinct from effects on checkpoint proteins, to enhance antitumor T‑cell activity alone or in combination with ICIs. Adults with advanced solid tumors received a range of doses of EIK1001 (QW IV) alone and in combination with pembrolizumab (200 mg Q3W; NCT03486301) or atezolizumab (1200 mg Q3W; NCT04196530) in Phase 1 studies (n=128). The linear, dose-proportional PK of EIK1001 is well described by the Pop-PK model. Increases in IFNγ and IP-10 were consistent with the anticipated mechanism of action, with doses representing target engagement identified. Further development of EIK1001 is underway."

Biomarker • Clinical • IO biomarker • P1 data • PK/PD data • Oncology • Solid Tumor • CXCL8 • IFNG • IL6 • TLR8

A Phase 2 Study of EIK1001 in Combination With Pembrolizumab and Chemotherapy in Patients With Stage 4 Non-Small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=70 | Recruiting | Sponsor: Eikon Therapeutics | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Phase 2 Study of EIK1001 in Combination With Pembrolizumab and Chemotherapy in Patients With Stage 4 Non-Small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=70 | Not yet recruiting | Sponsor: Eikon Therapeutics

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

BDB001-101: Clinical Study of BDB001 as a Mono-therapy or in Combination With Pembrolizumab (clinicaltrials.gov) - P1 | N=50 | Active, not recruiting | Sponsor: Eikon Therapeutics | Trial primary completion date: Dec 2023 ➔ Mar 2024

Combination therapy • Metastases • Trial primary completion date • Oncology • Solid Tumor

BDB001-102: Open Label Dose Escalation of BDB001 in Combination w Atezolizumab (clinicaltrials.gov) - P1 | N=40 | Active, not recruiting | Sponsor: Eikon Therapeutics | Trial primary completion date: Dec 2023 ➔ Mar 2024

Combination therapy • Metastases • Trial primary completion date • Oncology • Solid Tumor • CTLA4 • IL2 • TNFRSF9