The Future of Medicine

Why RNA Therapeutics?

ASOs have transformed RNA from "promising biology" into an engineered drug modality—pairing Watson–Crick targeting with drug-like chemistry and workable delivery routes.

10+
FDA-Approved ASOs
$5.8B
Market by 2025
100+
Clinical Trials Active

How ASOs Changed Everything

Three paradigm shifts that made RNA a practical drug target

RNA as a Drug Target

ASOs validated RNA as a practical, druggable target class—not a one-off success, but a repeatable modality with multiple approvals across diseases.

Key enabler: Chemical modifications (2′-MOE, PS backbone) that improved affinity, stability, and drug-like PK/PD.

Beyond Knockdown

ASOs expanded the "mechanism menu" beyond simple silencing. FDA now recognizes distinct mechanisms: splice modulation, RNase H cleavage, and more.

Example: Nusinersen doesn't silence—it restores SMN protein by fixing aberrant splicing.

CNS Delivery Unlocked

Nusinersen's success opened a credible path for neurodegeneration via intrathecal dosing—with learnings on delivery, tolerability, and biodistribution.

Impact: Distribution to CNS and peripheral tissues (muscle, liver, kidney) confirmed in autopsy data.
Clinical Proof Point

Nusinersen (SPINRAZA): The Flagship

The ASO that proved you can drug RNA with defined chemistry and achieve durable clinical benefit

Chemistry & Mechanism

Chemistry
2′-O-2-methoxyethyl (2′-MOE) sugar modifications + phosphorothioate (PS) backbone
Administration
Intrathecal delivery, 12 mg per dose, reaching CNS and peripheral tissues
Mechanism
Splice modulation: Increases exon 7 inclusion in SMN2 mRNA → restores full-length SMN protein production

Platform Implications

More than slowing decline
Nusinersen improves symptoms in symptomatic patients—not just stabilization, but improvement.
CNS program blueprint
Taught the field how to run CNS ASO programs: delivery, dosing, tolerability, biodistribution.
Route & tissue exposure
Operationalized that delivery route determines required safety assessments—now FDA guidance.
Repeatable chemistry
MOE/PS chemistry became a validated platform that other programs can build on.

Where ASOs Pushed the Field Next

The direction is clear: platform-driven development, not bespoke art projects

1

Privileged Chemistries

Marketed oligos converge on a limited set of chemical "families"—MOE, PS, LNA, PMO—reflecting workable platforms rather than endless optimization.

This convergence enables repeatable design rules, reusable analytics, and scalable discovery workflows.
2

Delivery as the Unlock

GalNAc conjugation enabled efficient hepatocyte delivery with robust, long-lasting silencing—up to 30× more potent vs unconjugated.

Delivery chemistry expands the therapeutic window and makes programs more practical.
3

Class-Aware Pharmacology

FDA recognizes oligos have unique PK/PD characteristics—minimal CYP modulation, route-driven distribution, distinct safety expectations.

This pushes toward systematic, platform-driven evaluation rather than ad hoc methods.
The Strategic Case

Why Jump on the ASO Ship Now?

What an ASO design platform buys you strategically

Mechanism-Aware Design

Splice modulators vs RNase H agents have different sequence constraints—FDA recognizes these categories.

Chemistry-Aware Optimization

Successful drugs repeatedly rely on MOE/PS—leverage validated chemistry classes, not reinvent.

Delivery/Route-Aware Selection

IT-CNS vs GalNAc-liver have very different distribution and safety implications—plan accordingly.

Portfolio Scalability

Many approved oligos across diseases support investing in a repeatable discovery engine.

If you want an RNA modality where design is rational and fast, chemistry is modular, and learnings transfer across programs—ASOs are the clearest validated path.

"ASOs shifted RNA therapeutics from 'promising biology' to an engineered drug modality—and the conditions now strongly favor building RNA/ASO design platforms rather than treating each ASO as a bespoke art project."