Rigel Pharmaceuticals (RIGL) investor relations material

Strategic growth and portfolio expansion

• Announced exclusive global in-licensing of VEPPANU (vepdegestrant), a first-in-class, FDA-approved oral PROTAC for ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer.

• VEPPANU is expected to become the largest commercial product and a major revenue driver, supporting transformational growth and leveraging existing commercial infrastructure.

• The transaction includes a $70M upfront payment, $15M in near-term milestones, up to $320M in additional milestones, and tiered royalties from mid-teens to mid-20s.

• Rigel gains global rights and is responsible for U.S. launch and commercialization, with sublicensing options internationally; agreement subject to regulatory clearance, expected to close mid-June 2026.

• Pfizer and Arvinas will continue ongoing development activities, with $40M support from Rigel over four years.

Clinical data and product differentiation

• VEPPANU demonstrated statistically significant and clinically meaningful improvement in progression-free survival (5.0 vs 2.1 months, HR 0.57, p<0.001) versus fulvestrant in ESR1-mutated patients.

• The pivotal VERITAC-2 phase III trial enrolled over 600 patients, all previously treated with endocrine therapy and CDK4/6 inhibitors.

• VEPPANU is the first and only FDA-approved oral PROTAC, offering a novel, catalytic mechanism for targeted ER degradation.

• The drug showed a favorable safety profile, with low rates of discontinuation (3%) and dose reduction (2%), and minimal severe GI toxicity; most adverse events were low grade.

• Most common side effects include decreased blood cells, increased liver enzymes, musculoskeletal pain, fatigue, nausea, decreased potassium, appetite loss, QT prolongation, and constipation; serious risks include QTc prolongation, requiring monitoring.

Regulatory and guideline milestones

• FDA approved VEPPANU on May 1, 2026, for adults with ER+/HER2-, ESR1-mutated advanced or metastatic breast cancer after at least one line of endocrine therapy.

• NCCN added vepdegestrant as a Category 2A treatment option in May 2026 for HR+/HER2-, ESR1-mutated advanced or metastatic breast cancer post-endocrine therapy and CDK4/6 inhibitor.

• Not recommended for children; pregnancy and breastfeeding precautions apply.