Radioligand therapy pairs a tumor-targeting molecule — often a peptide or peptide-adjacent scaffold — with a therapeutic radionuclide that delivers radiation directly to cancer cells. The class is anchored by two Novartis peptide-based products: Lutathera (lutetium-177 DOTATATE, a somatostatin-receptor peptide) for neuroendocrine tumors, and Pluvicto (lutetium-177 PSMA-617, a PSMA-targeting peptide) for metastatic castration-resistant prostate cancer. Pluvicto's expansion into pre-chemotherapy use in 2026 made it one of the fastest-growing oncology products.
The 2026 pipeline broadens the targeting-vector and radionuclide options. Telix Pharmaceuticals' ProstACT Global Phase 3 tests TLX591-Tx (lutetium-177 rosopatamab, a PSMA radio-antibody-drug conjugate) and met primary safety objectives in its Part 1 lead-in at ASCO 2026. Aktis Oncology's AKY-2519 is a B7-H3-targeting miniprotein radioconjugate with first-in-human imaging data at ASCO 2026. Crinetics' CRN09682 links a nonpeptide SSTR2 agonist to a cytotoxic payload, and Perspective Therapeutics brought its lead-212 (²¹²Pb) alpha-emitter platform to ASCO 2026 across VMT-α-NET in neuroendocrine tumors, VMT01 in melanoma, and PSV359 in solid tumors. The field spans peptide ligands, miniproteins, antibodies, and small molecules as the targeting vector, with lutetium-177, actinium-225, and lead-212 across the radionuclide options.
Stories here cover radioligand and radioconjugate trial readouts across PSMA, SSTR2, and B7-H3 targets. See #psma, #telix-pharmaceuticals, and #aktis-oncology for adjacent threads.
Lantheus's lutetium-177 dotatate ANDA (PNT2003), the first radioequivalent to Novartis's Lutathera, received FDA tentative approval on March 2, 2026; full approval is gated by the expiration of the 30-month Hatch-Waxman stay in June 2026. PNT2003 would launch into the gastroenteropancreatic neuroendocrine-tumor (GEP-NET) market alongside Lutathera and ahead of ITM-11 (Lu-edotreotide-177), which carries an August 28 PDUFA. Lantheus licensed PNT2003 from POINT Biopharma in December 2022, before Lilly's POINT acquisition.
The ASCO Annual Meeting closed June 2 after a week that moved peptide and targeted-conjugate oncology from abstract to podium: Bicycle's bicyclic peptide-drug conjugate and Avacta's FAP-activated conjugate in solid tumors, Mayo's folate-receptor and BioVaxys' survivin peptide vaccines, Sapience's C/EBPβ antagonist in glioblastoma, and PSMA and lead-212 radioligands from Telix and Perspective. Attention now shifts to ADA 2026 in New Orleans and the July 23-24 PCAC compounding vote.
Perspective Therapeutics presented progress on its three clinical lead-212 (²¹²Pb) targeted alpha-therapy programs at ASCO 2026: [212Pb]VMT-α-NET in somatostatin-receptor-2-positive neuroendocrine tumors, VMT01 in melanoma, and PSV359 in solid tumors. The NET program's earlier Phase 1/2a readout showed a 39% objective response rate in its second cohort and no dose-limiting toxicities at the 5.0 mCi dose, supporting movement toward a registrational trial. The platform pairs a peptide-based targeting vector with a short-range alpha emitter.
Telix Pharmaceuticals reported ProstACT Global Phase 3 Part 1 data at ASCO 2026 as a late-breaking presentation. TLX591-Tx (lutetium-177 rosopatamab tetraxetan) — a PSMA-targeted lutetium radio-antibody-drug conjugate — met its primary safety objectives in the safety and dosimetry lead-in, demonstrating an acceptable tolerability profile with no new safety signals when combined with enzalutamide (Xtandi), abiraterone (Zytiga), or followed by docetaxel in PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). ProstACT Global is an international Phase 3 trial evaluating TLX591-Tx plus standard of care versus standard of care alone. The drug sits in the PSMA-targeted radioligand class alongside Novartis's approved Pluvicto (lutetium-177 PSMA-617, a peptide-based radioligand), but uses an antibody rather than a small-molecule peptide as the targeting vector. The PSMA radioligand field — Pluvicto, ProstACT, plus the Aktis AKY-2519 B7-H3 miniprotein radioconjugate covered earlier this week — is one of the fastest-growing targeted-conjugate categories in oncology.
AlphaGen Therapeutics presented preclinical data at AACR 2026 (April 22) showing its novel macrocyclic peptide-based alpha-emitter radioligand [212Pb]Pb-AG1206 binds fibroblast activation protein with picomolar affinity, achieving rapid tumor accumulation, renal clearance, and a high tumor-to-kidney ratio. A sister candidate [212Pb]Pb-AG1002 targets SSTR2 as a non-agonist alpha therapy for neuroendocrine tumors.
Perspective Therapeutics' [212Pb]VMT-α-NET, a first-in-class alpha-emitter peptide radionuclide therapy targeting SSTR2, achieved objective responses in 10 of 23 (43%) Cohort 2 patients with metastatic neuroendocrine tumors in Phase 1/2a data presented at AACR 2026. 18 of 25 patients (72%) remained alive without progression; no dose-limiting toxicities or Grade 4/5 adverse events observed.