GB5121 / Gossamer Bio - LARVOL DELTA

STAR CNS: GB5121 in Adult Patients With Relapsed/Refractory CNS Lymphoma (clinicaltrials.gov) - P1b/2 | N=12 | Terminated | Sponsor: GB005, Inc., a wholly owned subsidiary of Gossamer Bio, Inc. | N=158 ➔ 12 | Trial completion date: Oct 2024 ➔ May 2023 | Active, not recruiting ➔ Terminated | Trial primary completion date: Oct 2024 ➔ May 2023; Sponsor decision

Enrollment change • Trial completion date • Trial primary completion date • Trial termination • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

STAR CNS: GB5121 in Adult Patients With Relapsed/Refractory CNS Lymphoma (clinicaltrials.gov) - P1b/2 | N=158 | Active, not recruiting | Sponsor: GB005, Inc., a wholly owned subsidiary of Gossamer Bio, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Gossamer Bio Inc. announces FDA has placed a partial clinical hold on all trials of GB5121 in response to serious adverse events (Investing.com) - "On April 3, 2023, Gossamer Bio, Inc...announced that the U.S. Food and Drug Administration (the 'FDA') has placed a partial clinical hold on all trials of GB5121, in response to serious adverse events that have been observed in the Phase 1b/2 STAR-CNS study, including atrial fibrillation, a sudden death event and a fatal intracranial hemorrhage....Based on the foregoing factors, the Company has decided to terminate all ongoing studies and discontinue development of GB5121."

Trial termination • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Gossamer Bio Announces Fourth Quarter and Full-Year 2022 Financial Results and Provides Business Update (Businesswire) - "GB5121: Oral, CNS-Penetrant BTK Inhibitor for Primary CNS Lymphoma (PCNSL): Based upon the benefit / risk profile observed to date and a prioritization of resources to support the seralutinib program, Gossamer has decided to pause enrollment in the Phase 1b/2 STAR CNS study. Gossamer plans to discuss available data with the study’s Data Review Committee to determine next steps."

P1/2 data • Trial status • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

A PHASE 1B/2 STUDY OF GB5121, A NOVEL, HIGHLY SELECTIVE, POTENT, AND CNS-PENETRANT BTK INHIBITOR FOR RELAPSED/REFRACTORY PRIMARY/SECONDARY CNS LYMPHOMA AND PRIMARY VITREORETINAL LYMPHOMA (EHA 2022) - P1b/2 | "GB5121 is a novel, orally available, covalent BTKi, which has shown superior specificity, CNS penetration, and CNS target occupancy in preclinical testing compared to other BTKis including ibrutinib...This clinical trial is anticipated to start enrollment in May 2022. Results N/A (trial in progress) Conclusion N/A (trial in progress)"

P1/2 data • Bone Marrow Transplantation • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Transplantation

Trial in Progress: A Phase 1b/2 Study of GB5121, a Brain-Penetrant, Potent, Highly Selective, and Irreversible BTK Inhibitor for Relapsed/Refractory Primary/Secondary CNS Lymphoma and Primary Vitreoretinal Lymphoma (ASH 2022) - P1b/2 | "Ibrutinib, a first-generation BTK inhibitor (BTKi), has been evaluated in two phase 1/2 trials for relapsed/refractory primary/secondary CNS lymphoma (R/R PCNSL, SCNSL) and primary vitreoretinal lymphoma (PVRL) showing limited survival benefit...Progression-free survival and overall survival will be evaluated. This clinical trial started enrollment in May 2022.Result s : N/A (trial in progress) Conclusion s : N/A (trial in progress)"

P1/2 data • Bone Marrow Transplantation • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Disorders • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Transplantation

Safety, Tolerability, and Pharmacokinetic Profile of Single and Multiple Ascending Doses of GB5121, a CNS-Penetrant BTK Inhibitor, in Healthy Subjects (ASH 2022) - P1b/2 | "PD analysis and additional evaluations are ongoing and final results will be presented. The safety and PK profiles of GB5121 support its continued evaluation in the ongoing Phase 1b/2 open-label, international study in adult subjects with relapsed/refractory primary/secondary CNS lymphoma, or primary vitreoretinal lymphoma (STAR CNS; NCT05242146)."

Clinical • PK/PD data • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Disorders • Hematological Malignancies • Lymphoma • Oncology

GB5121, a Brain-Penetrant, Irreversible BTK Inhibitor, Demonstrates Potent Anti-Tumor Activity in a Novel Mouse Model of Intracranial Lymphoma (ASH 2022) - P1b/2 | "GB5121 was designed to be a brain-penetrant BTKi; a PET imaging study confirms the results of previously conducted NHP PK studies demonstrating CNS penetration of GB5121. In a novel model of intracranial lymphoma, treatment with GB5121 resulted in better anti-tumor activity compared to ibrutinib, likely resulting from higher brain penetration and TO. This higher brain penetration and TO exhibited by GB5121 may result in more durable responses in malignancies with CNS involvement and supports the investigation of GB5121 in clinical trials for CNS lymphomas."

Preclinical • CNS Lymphoma • Hematological Disorders • Hematological Malignancies • Immunology • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • CD20 • IL10

GB5121 is a novel, irreversible, covalent BTK inhibitor with high selectivity and CNS-penetrance for treatment of CNS malignancies (SNO 2022) - "Here, GB5121 was profiled for selectivity, potency, inactivation kinetics and CNS penetrance in comparison to ibrutinib. Our data supports the use of GB5121 in clinical trials where BTK is a known driver of malignancies, including CNS lymphoma. This research has been previously presented at the AACR Annual Meeting 2022."

Brain Cancer • CNS Disorders • CNS Lymphoma • CNS Tumor • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • EGFR

Trial in Progress: A Phase 1b/2 Study of GB5121, a Novel, Highly Selective, Potent, and CNS-Penetrant BTK Inhibitor for Relapsed/Refractory Primary/Secondary CNS Lymphoma and Primary Vitreoretinal Lymphoma (PPLC 2022) - P1b/2 | "N/A (trial in progress)"

P1/2 data • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Gossamer Bio Announces Second Quarter 2022 Financial Results and Provides Business Update (GlobeNewswire) - "GB5121: Oral, CNS-Penetrant BTK Inhibitor for Primary CNS Lymphoma (PCNSL) and other Rare CNS Malignancies: First patient dosed in Phase 1b/2 STAR CNS Study in relapsed / refractory PCNSL and other rare CNS malignancies; Results from open-label Phase 1b/2 STAR CNS to be presented at relevant medical conferences, as data become available."

New P1/2 trial • Trial status • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

GB5121 Is a Novel, Irreversible, Covalent BTK Inhibitor with High Selectivity and CNS-Penetrance for Treatment of CNS Malignancies (PPLC 2022) - "Here, GB5121 was profiled for selectivity, potency, inactivation kinetics and CNS penetrance in comparison to ibrutinib. The unique profile of GB5121 provides differentiation from both FDA-approved BTK inhibitors and those currently under clinical investigation. Our data supports the use of GB5121 in clinical trials where BTK is a known driver of malignancies, including CNS lymphoma. This research has been previously presented at the AACR Annual Meeting 2022."

CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • EGFR

GB5121 IS A NOVEL, IRREVERSIBLE, COVALENT BTK INHIBITOR WITH HIGH SELECTIVITY AND CNS-PENETRANCE FOR TREATMENT OF CNS MALIGNANCIES (EHA 2022) - "Aims To profile GB5121 for selectivity, potency, inactivation kinetics and CNS penetrance in comparison to ibrutinib. Our data supports the use of GB5121 in clinical trials where BTK is a known driver of malignancies, including in CNS lymphoma. This research has been previously presented at the AACR Annual Meeting 2022."

Brain Cancer • CNS Disorders • CNS Lymphoma • CNS Tumor • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • EGFR

STAR CNS: GB5121 in Adult Patients With Relapsed/Refractory CNS Lymphoma (clinicaltrials.gov) - P1b/2 | N=158 | Recruiting | Sponsor: GB005, Inc., a wholly owned subsidiary of Gossamer Bio, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Gossamer Bio Announces First Quarter 2022 Financial Results and Provides Business Update (Businesswire) - "We expect to initiate the Phase 1b/2 STAR CNS Study in relapsed / refractory PCNSL and other rare CNS malignancies in the second quarter of 2022."

Enrollment status • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

GB5121 is a novel highly potent and selective CNS-penetrant BTK inhibitor for CNS malignancies (AACR 2022) - "Specifically, GB5121 showed ~2-fold higher brain concentrations with lower plasma levels than ibrutinib. Together, these features differentiate GB5121 from both FDA-approved BTK inhibitors as well as those currently under clinical investigation. Our data supports the use of GB5121 in clinical trials where BTK is a known driver of malignancies, including in CNS lymphoma."

Brain Cancer • CNS Lymphoma • CNS Tumor • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • EGFR

Gossamer Bio Announces Third Quarter 2021 Financial Results and Provides Corporate Update (Businesswire) - "GB5121: Oral, Covalent, CNS-Penetrant BTK Inhibitor for Primary CNS Lymphoma (PCNSL): First subject dosed in first-in-human Phase 1 clinical trial in healthy volunteers."

Trial status • Oncology

Gossamer Bio Announces Addition of Two CNS-Penetrant BTK Inhibitors to its Product Candidate Pipeline: GB5121 & GB7208 (Businesswire) - "Gossamer Bio, Inc....announced the addition of two CNS-penetrant Bruton’s tyrosine kinase (BTK) inhibitors to its product candidate pipeline....Gossamer plans to initiate first-in-human studies of the first of these candidates, GB5121, in the fourth quarter of 2021. Gossamer intends to develop GB5121 in CNS-oncology indications, including relapsed / refractory primary CNS lymphoma (PCNSL), for which a potentially registrational Phase 1b / 2 study is expected to initiate in the first half of 2022."

New P1/2 trial • Pipeline update • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Gossamer Bio Announces Addition of Two CNS-Penetrant BTK Inhibitors to its Product Candidate Pipeline: GB5121 & GB7208 (Businesswire) - "Gossamer Bio, Inc...announced the addition of two CNS-penetrant Bruton’s tyrosine kinase (BTK) inhibitors to its product candidate pipeline. Gossamer plans to initiate first-in-human studies of the first of these candidates, GB5121, in the fourth quarter of 2021. Gossamer intends to develop GB5121 in CNS-oncology indications, including relapsed / refractory primary CNS lymphoma (PCNSL), for which a potentially registrational Phase 1b / 2 study is expected to initiate in the first half of 2022."

New P1/2 trial • CNS Lymphoma • Hematological Malignancies • Oncology