GS-8824 / Gilead - LARVOL DELTA

NAPISTAR 1-01: A phase I dose escalation study of TUB-040, a novel NaPi2b-targeting exatecan antibody-drug conjugate (ADC) in patients with platinum-resistant ovarian (PROC) high grade serous carcinoma (HGSC) (ESMO 2025) - P1/2 | "Pts had a median age of 62 y (range 34-81), ECOG PS 0 or 1, a median of 4 prior lines of therapy (range 1-7); prior treatment included bevacizumab (84%), PARP inhibitors (76%) and mirvetuximab soravtansine (13%). 1 Values reported with 95% CI. Conclusions TUB-040 was well tolerated with robust clinical activity even at low doses, offering a differentiated potential new option for treatment with a highly favorable benefit–risk profile."

Clinical • Late-breaking abstract • P1 data • Platinum resistant • Lung Cancer • Non Small Cell Lung Cancer • Oncology • MUC16 • SLC34A2

NAPISTAR 1-01: Results of phase 1 dose escalation of monotherapy with TUB-040, a novel NaPi2b-targeting exatecan ADC, in patients (pts) with platinum-resistant ovarian cancer (PROC). (ASCO 2026) - P1/2 | "Median age: 62 years (34-81), ECOG PS 0-1, median prior lines: 4 (1-7), prior treatment included bevacizumab (84%), PARPi (76%), and mirvetuximab soravtansine (13%). TUB-040 was well tolerated with promising clinical activity at low doses, offering a potential new treatment option with a differentiated, favorable benefit–risk profile and a wide therapeutic window in PROC pts. Dose optimization is currently ongoing."

ADC • Clinical • Monotherapy • P1 data • Platinum resistant • Alopecia • Constipation • Gastroenterology • Gastrointestinal Disorder • High Grade Serous Ovarian Cancer • Immunology • Lung Cancer • Neutropenia • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Pneumonia • Solid Tumor • MUC16 • SLC34A2

UPDATED RESULTS AND BIOMARKER-RELATED EFFICACY FOR PHASE 1 DOSE ESCALATION OF TUB-040, A NOVEL NAPI2B-TARGETING EXATECAN ANTI-BODY DRUG CONJUGATE IN PATIENTS WITH PLATINUM-RESISTANT OVARIAN CANCER (IGCS 2026) - "Introduction: TUB-040 is a DAR8 ADC targeting NaPi2b, overexpressed in ovarian, endometrial and NSCLC, and comprising a humanized Fc -silenced IgG1 mAb conjugated to exatecan via a cleavable, cysteine -selective, stable, solubility -mediating P5 linker providing excellent stability and biophysical properties. As of April 5, 2026, 67 PROC pts received TUB -040 for a median of 12 cycles with 32 (48%) pts still ongoing. Median age 62 years (34 -81), median 4 prior lines (1 -7), prior treatment with BEV (84%), PARPi (76%), immunotherapy (24%), and mirvetuximab soravtansine (15%). The most common all grade TEAEs were nausea (76%), fatigue (60%), neutropenia (54%), anemia (48%), constipation (37%), diarrhea (31%), vomiting (31%), and alopecia (31%)."

ADC • Biomarker • Clinical • IO biomarker • P1 data • Platinum resistant • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2

Study of TUB-040 in Participants With Unresectable or Metastatic Nonsquamous Non-small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=80 | Not yet recruiting | Sponsor: Tubulis GmbH

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

Has next-generation antibody-drug conjugate engineering finally unlocked NaPi2b in ovarian cancer? (PubMed, Int J Gynecol Cancer) - No abstract available

Journal • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2

NAPISTAR 1-03: Study of TUB-040 in Patients With Recurrent or Progressive Uterine Cancer After Chemotherapy and Immune Therapy (clinicaltrials.gov) - P1/2 | N=100 | Not yet recruiting | Sponsor: Tubulis GmbH

Checkpoint inhibition • dMMR • MSI-H • New P1/2 trial • Endometrial Cancer • Oncology • Solid Tumor • Uterine Cancer • PD-L1 • SLC34A2

OC: Study of TUB-040 Given With Standard Ovarian Cancer Drugs in Patients With Fast-growing Ovarian Cancer (clinicaltrials.gov) - P1/2 | N=72 | Recruiting | Sponsor: Tubulis GmbH

New P1/2 trial • Platinum sensitive • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor

GS-8824: Initiated P1 NAPISTAR-1-02 Study in 2L-3L PSOC Patients (Gilead) - "Registrational Trial Initiation Expected in 2027"

New trial • Platinum sensitive • Trial status • Ovarian Cancer

NAPISTAR1-01: FiH Study to Investigate Safety, PK and Efficacy of the NaPi2b ADC TUB-040 in Patients With PROC or r/r Adenocarcinoma NSCLC (clinicaltrials.gov) - P1/2 | N=100 | Recruiting | Sponsor: Tubulis GmbH | Not yet recruiting ➔ Recruiting

Enrollment open • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor

Gilead Sciences Completes Acquisition of Tubulis Further Strengthening Oncology Portfolio (Businesswire) - "The acquisition brings Gilead next-generation ADC assets and a platform designed to maximize patient benefit through more selective delivery of diverse payloads to tumors....The addition of Tubulis’ lead asset, TUB-040, a NaPi2b-directed topoisomerase-I inhibitor (TOPO1i) ADC, which has demonstrated promising activity in platinum-resistant ovarian cancer, and TUB-030, a 5T4-directed ADC that is being investigated across various solid tumor types, complements Gilead’s existing ADC portfolio....Under the terms of the agreement, Gilead acquired all the outstanding equity of Tubulis for $3.15 billion in upfront considerations on a cash-free, debt-free basis, and up to $1.85 billion in contingent milestone payments."

M&A • Platinum resistant • Ovarian Cancer

Key Updates Since Our Last Quarterly Release:…Oncology (Businesswire) - "Announced a definitive agreement to acquire Tubulis, a private clinical-stage biotechnology company developing next-generation antibody-drug conjugates ('ADC'), including lead asset TUB-040, a NaPi2b-directed topoisomerase-I inhibitor ADC currently in Phase 1b/2 development for platinum-resistant ovarian cancer and non-small cell lung cancer. Closing of the transaction is subject to expiration or termination of certain regulatory filings and other customary conditions."

M&A • Platinum resistant • Non Small Cell Lung Cancer • Ovarian Cancer

NAPISTAR1-01: FiH Study to Investigate Safety, PK and Efficacy of the NaPi2b ADC TUB-040 in Patients With PROC or r/r Adenocarcinoma NSCLC (clinicaltrials.gov) - P1/2 | N=250 | Recruiting | Sponsor: Tubulis GmbH | N=174 ➔ 250

Enrollment change • First-in-human • Platinum resistant • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2

Tubulis…announced that an abstract covering current clinical trial data from its ongoing Phase I/IIa NAPISTAR 1-01 trial (NCT06303505) has been accepted for a rapid oral presentation at the upcoming American Society of Clinical Oncology (ASCO) Meeting (Businesswire) - "The presentation...will provide an update of maturing data from the ongoing dose escalation part of the ovarian cancer cohort."

P1 data • Platinum resistant • Ovarian Cancer

NAPISTAR1-01: FiH Study to Investigate Safety, PK and Efficacy of the NaPi2b ADC TUB-040 in Patients With PROC or r/r Adenocarcinoma NSCLC (clinicaltrials.gov) - P1/2 | N=174 | Recruiting | Sponsor: Tubulis GmbH | N=120 ➔ 174

Enrollment change • First-in-human • Platinum resistant • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Refractory Ovarian Cancer • Solid Tumor • ALK • BRAF • FOLR1 • HER-2 • KRAS • MET • NTRK • RET • ROS1 • SLC34A2

TUB-040, a novel Napi2b-targeting ADC built with ethynylphosphonamidate conjugation chemistry, demonstrates high and long-lasting anti-tumor efficacy via Topoisomerase-I inhibition and excellent tolerability predictive of a wide therapeutic window in humans (AACR 2024) - "Allometric scaling and PK/PD modelling predicts a human serum half-life greater 10 days and a therapeutic index in humans up to 55. Based on these results, TUB-040, designed with differentiating technology for optimal efficacy and tolerability, is ready for testing in clinical trials."

ADC • Clinical • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2 • TOP1

Gilead to Acquire Tubulis Adding Potentially Best-in-Class Antibody-Drug Conjugate and Next Generation Platform to Further Strengthen Oncology Pipeline (Businesswire) - "Acquisition Adds TUB-040, a NaPi2b Targeting ADC for Ovarian Cancer and other Solid Tumors, to Gilead Pipeline....Gilead will also acquire TUB-030, a 5T4 targeted ADC, which has demonstrated promising initial clinical data across various solid tumor types....Closing of the transaction is subject to expiration or termination of certain regulatory filings and other customary conditions. The transaction is expected to close in the second quarter of 2026."

Licensing / partnership • Platinum resistant • Non Small Cell Lung Cancer • Ovarian Cancer

NAPISTAR 1-02: A Study Testing a New Targeted Drug (TUB-040) in combination with Standard Chemotherapy for Women with Ovarian Cancer (clinicaltrialsregister.eu) - P1/2 | N=42 | Recruiting | Sponsor: Tubulis GmbH | Not yet recruiting ➔ Recruiting

Enrollment open • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor • BRCA • BRCA1 • BRCA2 • HRD • SLC34A2

NAPISTAR 1-01: A Phase 1 dose escalation study of TUB-040, a novel NaPi2b-targeting exatecan antibody-drug conjugate in patients with platinum-resistant high grade serous ovarian carcinoma. (ESGO 2026) - "Median age 62 years (34-81), median 4 prior lines (1-7), prior treatment included bevacizumab (84%), PARPi (76%), mirvetuximab soravtansine (13%). The cDCR was 96% [95% CI, 85-99]. Among CA-125 evaluable patients, GCIG CA-125 response occurred in 81% (34/42) and 96% (24/25) of RECIST responders achieved a CA-125 response.Conclusion TUB-040 was well tolerated with very promising clinical activity at low doses, offering a potential new option for treatment with a differentiated, highly favourable benefit–risk profile."

Clinical • P1 data • Platinum resistant • High Grade Serous Ovarian Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • MUC16 • SLC34A2

NAPISTAR1-01: FiH Study to Investigate Safety, PK and Efficacy of the NaPi2b ADC TUB-040 in Patients With PROC or r/r Adenocarcinoma NSCLC (clinicaltrials.gov) - P1/2 | N=250 | Recruiting | Sponsor: Tubulis GmbH | Trial completion date: Jan 2027 ➔ Dec 2027 | Trial primary completion date: Jan 2027 ➔ Dec 2027

First-in-human • Platinum resistant • Trial completion date • Trial primary completion date • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2

NAPISTAR 1-02: A Study Testing a New Targeted Drug (TUB-040) in combination with Standard Chemotherapy for Women with Ovarian Cancer (clinicaltrialsregister.eu) - P1/2 | N=42 | Not yet recruiting | Sponsor: Tubulis GmbH

New P1/2 trial • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor • BRCA • BRCA1 • BRCA2 • HRD • SLC34A2

NAPISTAR 1-01: A Phase 1 dose escalation study of TUB-040, a novel NaPi2b-targeting exatecan antibody-drug conjugate in patients with platinum-resistant high grade serous ovarian carcinoma. (ESGO 2026) - "Median age 62 years (34-81), median 4 prior lines (1-7), prior treatment included bevacizumab (84%), PARPi (76%), mirvetuximab soravtansine (13%). The cDCR was 96% [95% CI, 85-99]. Among CA-125 evaluable patients, GCIG CA-125 response occurred in 81% (34/42) and 96% (24/25) of RECIST responders achieved a CA-125 response.Conclusion TUB-040 was well tolerated with very promising clinical activity at low doses, offering a potential new option for treatment with a differentiated, highly favourable benefit–risk profile."

Clinical • P1 data • Platinum resistant • High Grade Serous Ovarian Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • MUC16 • SLC34A2

NAPISTAR1-01: FiH Study to Investigate Safety, PK and Efficacy of the NaPi2b ADC TUB-040 in Patients With PROC or r/r Adenocarcinoma NSCLC (clinicaltrials.gov) - P1/2 | N=200 | Recruiting | Sponsor: Tubulis GmbH | N=100 ➔ 200

Enrollment change • First-in-human • Platinum resistant • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor

Tubulis Raises €308 Million Series C to Accelerate Clinical Development of Lead ADC Candidate TUB-040 and Expand Pipeline (Yahoo Finance) - "The proceeds from the Series C financing will be used to expand the clinical development of TUB-040, Tubulis’ lead antibody-drug conjugate (ADC) candidate, into earlier lines of therapy and additional tumor indications....The capital will also advance Tubulis’ pipeline, including the clinical-stage ADC candidate TUB-030, several preclinical programs, and expand its proprietary ADC platform technologies to bring ADCs into novel applications."

Financing • Platinum resistant • Non Small Cell Lung Cancer • Ovarian Cancer

Tubulis Presents First Clinical Data from Phase I/IIa Trial for TUB-040 in Platinum-Resistant Ovarian Cancer (PROC) at ESMO 2025 (Businesswire) - "Within the 1.67-3.3 mg/kg dose cohorts, an ORR of 59% (range of 50-67%), was achieved with a confirmed ORR of 50%; one complete response (CR) was observed at 2.5 mg/kg. Treatment is ongoing in 80% of patients within the 1.67 – 3.3 mg/kg cohorts and in 93% of all responding patients from this focus group; The confirmed disease control rate (DCR) at 1.67 – 3.3 mg/kg was 96% and a confirmed DCR of 91% was reached across all cohorts at the data-cut-off with efficacy data in the 3.3 mg/kg group still continuing to mature."

Late-breaking abstract • P1/2 data • Platinum resistant • Ovarian Cancer

NAPISTAR 1-01: An International Phase I/II Trial of the Novel ADC TUB-040 in Advanced/Metastatic NSCLC Adenocarcinoma (IASLC-WCLC 2025) - P1/2 | "The dose-escalation framework includes initial double-dosing steps with a 100% increment over the standard dose, transitioning to modified Fibonacci increments (67%, 50%, and 33% dose increments) with intra-patient escalation permissible at low exposure levels. Phase IIa involves the randomization of patients for dose optimization at two or more doses to further characterize the safety profile and identify the optimal therapeutic dose."

Metastases • P1/2 data • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • SLC34A2