Ionis enters exclusive licensing agreement with Bicycle Therapeutics aimed at further advancing LICA technology

- Exclusive rights to innovative peptide technology positions Ionis to further strengthen targeting capabilities of its LICA therapies

CARLSBAD, CA, USA I July 13, 2021 I Ionis Pharmaceuticals, Inc. (NASDAQ: IONS) today announced that it has entered into an exclusive licensing agreement with Bicycle Therapeutics plc (NASDAQ: BCYC) to increase the delivery capabilities of Ionis' advanced LIgand Conjugated Antisense (LICA) medicines. The agreement provides Ionis exclusive access to Bicycle's proprietary macrocyclic peptides, referred to as Bicycles, to design LICAs that target transferrin receptor 1 for use with oligonucleotides. This LICA strategy has demonstrated both the improved delivery of antisense medicines to muscle tissue, including cardiac muscle, as well as the potential to cross the blood brain barrier.

Bicycle Therapeutics is a clinical-stage biopharmaceutical company developing a novel class of medicines, Bicycles, for diseases that are underserved by existing therapeutics. Bicycles are fully synthetic short peptides constrained with small molecule scaffolds to form two loops that stabilize their structural geometry. This constraint facilitates target binding with high affinity and selectivity, making Bicycles attractive candidates for drug development.

"One of our key strategic objectives is to expand our drug discovery capabilities. The agreement with Bicycle Therapeutics represents a strategic addition to our expanding LICA platform, giving us the potential to meaningfully expand our drug discovery capabilities and deliver many more transformational medicines to the market," said Brett P. Monia, Ph.D., Ionis' chief executive officer. "We believe that investing in technologies like Bicycle's cutting-edge transferrin receptor 1-targeting peptides will enhance our ability to design medicines to tackle devastating diseases in need of better treatment options."

"Our collaboration with Bicycle will accelerate Ionis' progress toward creating best-in-class, low molecular weight ligands for muscle-specific targeted delivery," said Eric E. Swayze, Ph.D., executive vice president of research at Ionis. "This approach offers several potential advantages over related strategies in development, including increased potency, more convenient administration, less complex manufacturing processes and reduced cost of goods." Dr. Swayze added, "We are pleased with the data we have generated to date and look forward to incorporating optimized Bicycle peptides into our LICA delivery platform."

Under terms of the agreement, Ionis obtained an exclusive license to Bicycle's technology covering the entire class of transferrin receptor 1 Bicycles for use in targeted delivery of oligonucleotide drugs. Ionis made a $45 million upfront payment to Bicycle which included a license fee, an option fee, and an $11 million equity investment in Bicycle. Bicycle will be eligible to earn development and regulatory milestone payments on a program-by-program basis and royalties on product sales.

About Ionis Pharmaceuticals, Inc.

For more than 30 years, Ionis has been the leader in RNA-targeted therapy, pioneering new markets and changing standards of care with its novel antisense technology. Ionis currently has three marketed medicines and a premier late-stage pipeline highlighted by industry-leading neurological and cardiometabolic franchises. Our scientific innovation began and continues with the knowledge that sick people depend on us, which fuels our vision of becoming one of the most successful biotechnology companies.

To learn more about Ionis visit www.ionispharma.com and follow us on Twitter @ionispharma.

SOURCE: Ionis Pharmaceuticals

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