Blog - TD2 Precision Oncology

Why Small Molecules Are Still a Big Deal

Written by TD2 Admin | April 8, 2025 at 11:06 AM

In the biotech world, small molecules often get treated like the veteran actor at the awards show – respected, but no longer the star of the night. With the spotlight focused on cell therapies, biologics, and antibody-drug conjugates, it’s easy to assume small molecules are yesterday’s news. But don’t let their modest size or long-standing presence fool you. These molecular workhorses are still doing the heavy lifting in oncology, and they’re not done yet.

Proven Modality with Broad Applicability

Small molecules have a decades-long track record of clinical success in oncology. From kinase inhibitors to hormone therapies, they have consistently delivered efficacy across a wide spectrum of cancers. Their ability to enter cells and act on intracellular targets, many of which are currently inaccessible to larger biologics, makes them uniquely valuable in targeting the molecular underpinnings of cancer.

Superior Accessibility and Scalability

Small molecules are often orally available, easier to manufacture, and more cost-effective than biologics. These attributes not only benefit healthcare systems and patients but also provide biotech companies with scalable treatment platforms that are easier to commercialize globally. For indications requiring chronic treatment, small molecules often offer a more convenient and sustainable option.

Innovation Is Far from Over

The field of small molecule oncology is experiencing a resurgence of innovation. Advances in structure-based drug design, AI-powered screening, and novel modalities such as targeted protein degradation (e.g., PROTACs) are pushing the boundaries of what small molecules can do. These technologies allow for more selective targeting, reduced toxicity, and the ability to overcome resistance mechanisms, hallmarks of next-generation cancer therapies.

Synergy with Complex Modalities

Rather than competing with biologics and cell therapies, small molecules often complement them. Combination therapies using small molecules can enhance the efficacy of immunotherapies or mitigate resistance in targeted biologics. Their role in the treatment ecosystem is dynamic and synergistic – not outdated.

A Lower Barrier to Entry for Innovation

For early-stage biotech companies, developing small molecules can be more feasible than embarking on biologics or cell therapy programs. Lower manufacturing costs, more straightforward regulatory pathways, and a wider base of clinical experience make small molecule development an attractive avenue for innovation.

Small molecules may be compact, but their impact on oncology is anything but small. Now is not the time to move on; it’s the time to move forward.

Ready to take your small molecule program to the next phase? Contact TD2 Oncology to learn how we can accelerate your clinical development.