Radioligand therapies (RLT) deliver targeted radiation to tumors by linking radioactive isotopes to targeting molecules—small molecules, peptides, or antibodies—while minimizing damage to healthy tissue.

The field widely adopts a theranostic approach: imaging first confirms target uptake, and only patients with positive scans receive treatment.

Radioactive iodine has been used to treat thyroid diseases since the 1940s, but major breakthroughs in oncology came decades later.

Peptide receptor radionuclide therapy (PRRT) marked a key advance for neuroendocrine tumors. By targeting somatostatin receptor‑expressing cancer cells with radiolabeled somatostatin analogs, lutetium‑177 dotatate (Lutathera) was approved in the U.S. in 2018.

The field then expanded into prostate cancer, with therapies targeting prostate‑specific membrane antigen (PSMA)—a protein highly expressed in prostate tumors—emerging as an ideal target.

By 2025, the radioligand therapy landscape had largely consolidated. The most transformative shift was not proving RLT efficacy, but a dramatic move to earlier lines of therapy.

The label expansion of Pluvicto signaled that RLT was no longer confined to late‑line settings, but entering earlier treatment sequences. In short, radioligand therapy is emerging as a mainstream cancer treatment.

The PSMAdition trial reinforced this trend. It evaluated Pluvicto plus standard hormone therapy in metastatic hormone‑sensitive prostate cancer (mHSPC).

Novartis reported that in a pre‑specified interim analysis, the combination arm achieved statistically significant and clinically meaningful improvement in radiographic progression‑free survival. If approved, RLT would stand alongside first‑line hormone therapy, not just as a later salvage option.

Another key signal in 2025 was the shift in capital flow.

Investors moved beyond chasing a few promising candidates and began funding large‑scale industrialization. Several large private financing rounds that year explicitly allocated capital to isotope access, manufacturing network expansion, and platform capabilities—not just single clinical programs.

• Swiss radiopharma company Nuclidium raised a CHF 79 million (≈ $98 million) Series B in July to advance its copper‑based theranostic pipeline and expand manufacturing infrastructure in Europe and the U.S.
• A day later, Actithera closed an oversubscribed $75.5 million Series A to advance fibroblast activation protein (FAP)‑targeted radioligand programs and its discovery platform.
• ARTBIO raised $132 million in a Series B round dedicated to building its alpha‑emitting radioligand pipeline and isotope supply and manufacturing capacity.
• AdvanCell completed a $112 million Series C in early 2025 to advance clinical programs and scale targeted alpha therapy production.

The unique nature of the radiopharmaceutical market makes it a high‑barrier game. Unlike conventional drugs, radiopharmaceutical R&D spans nuclear physics, radiochemistry, oncology, and pharmaceutical development, with strict radioactive material regulations.

According to Evaluate Pharma, the global radiopharmaceutical market reached approximately $10 billion in 2023 and is projected to grow to $30 billion by 2030.

Radiopharmaceuticals for cancer represent the largest segment, especially in prostate cancer, neuroendocrine tumors, and lymphoma.

Novartis is the clear leader, having built a comprehensive radiopharma footprint through a series of targeted acquisitions. In 2017, it bought Advanced Accelerator Applications for $3.9 billion to gain Lutathera. In 2018, it acquired Endocyte for $2.1 billion, securing Pluvicto—now a blockbuster.

These investments are delivering strong returns. In 2025, Pluvicto generated $1.99 billion in annual sales, up 42% year‑over‑year; Lutathera recorded $816 million. Novartis expects Pluvicto to exceed $5 billion in peak sales, positioning it as one of the most successful radiopharmaceuticals ever.

Novartis continues to expand Pluvicto’s label—adding pre‑chemotherapy mCRPC in March 2025, with positive mHSPC Phase III data recently disclosed. It is also building an alpha‑emitting portfolio and researching combinations of beta and alpha emitters. Through multiple acquisitions, Novartis has broadened its pipeline across tumor types, extending RLT into lung, breast, and other common solid tumors.

AstraZeneca has taken a differentiated catch‑up path.

In March 2024, it acquired Fusion Pharmaceuticals for an aggregate transaction value of roughly $2.4 billion, gaining multiple clinical‑stage radiopharmaceuticals including FPI‑2265—a PSMA‑targeted RLT using actinium‑225, an alpha emitter. This creates a technical divergence from Pluvicto, which uses the beta emitter lutetium‑177.

Alpha and beta emitters represent two distinct technological tracks. Alpha particles have greater mass and higher energy, causing more efficient DNA double‑strand breaks, but also pose greater safety challenges. AstraZeneca’s bet on alpha emitters aims to secure leadership in next‑generation radiopharmaceuticals.

Eli Lilly’s entry has been more aggressive.

Its acquisition of Point Biopharma delivered PNT2002 and other candidates, rapidly filling its PSMA‑targeted portfolio while exploring multiple tumor types and technologies. In February 2025, Lilly entered a strategic collaboration with AdvanCell, integrating lead‑212 production and isotope development facilities to advance targeted alpha therapies.

Lilly’s radiopharma pipeline now spans RLT, alpha emitters, and RDCs across multiple cancers, turning it from a newcomer into a formidable competitor.

Beyond these giants, Bayer holds a strong position with Xofigo (radium‑223), approved for metastatic castration‑resistant prostate cancer. It maintains a significant global share based on its demonstrated efficacy.

The FDA review of ITM‑11 (Lu‑edotreotide‑177) for gastroenteropancreatic neuroendocrine tumors (NETs) is closely watched, with a target action date of August 28, 2026.

If approved, ITM‑11 will break Lutathera’s exclusive hold on the PRRT market since 2018, expanding treatment options for NET patients.

After Pluvicto’s shift to earlier lines, the field is focused on maturing data in earlier treatment settings.

Novartis’s PSMAdition trial showed striking radiographic progression‑free survival benefit, but overall survival data remain immature. Further readouts in 2026 will help define RLT’s role and durability in first‑line mHSPC.

Big pharma has clearly pivoted to alpha‑emitter therapies, as seen in BMS’s acquisition of RayzeBio and AstraZeneca’s purchase of Fusion. RayzeBio’s RYZ101 and Fusion’s FPI‑2265 are both in late‑stage development.

Key 2026 milestones will go beyond early response rates: they include establishing tolerability, validating repeat dosing, and scaling alpha‑isotope supply. Solidifying this evidence will support broader clinical adoption of alpha‑emitter therapies.

Whether radioligand therapies can move beyond PSMA and somatostatin receptors will be a critical measure of the field’s long‑term potential. Of keen interest is whether emerging targets will demonstrate reliable imaging selection, consistent tumor uptake, and manageable safety profiles in large‑scale trials.

The sensitivity of radioligand therapies to isotope half‑life means scaling will depend heavily on robust production and distribution networks.

As more programs advance into late‑stage development and earlier lines of therapy, cross‑site drug delivery capacity will become increasingly critical. Expect more strategic partnerships and investments focused on industrial infrastructure in 2026.