A Phase 1 Open-Label, First-in-human, Dose Escalation and Expansion Study to Determine the Safety, Tolerability, Dosimetry, Pharmacokinetics, and Preliminary Efficacy of 212Pb-DOTAM-GRPR1 in Adult Participants with Recurrent or Metastatic GRPR-expressing Tumors
Metastatic castration-resistant prostate cancer (mCRPC) including neuroendocrine prostate cancer (NEPC) (enrolled only in SAD and MAD Q6W)
HR+/HER2- breast cancer (estrogen receptor/ER expression >10% of tumor cell nuclei stain, regardless of progesterone receptor/PgR expression); HER2-negative including HER2-low (as per relevant ASCO/CAP guidelines)
Colorectal cancer
Cervical cancer
None
Single group
²¹²Pb-DOTAM-GRPR1
Drug²¹²Pb-DOTAM-GRPR1 is a radioimmunoconjugate comprised of ²¹²Pb, the metal chelator DOTAM (1,4,7,10-Tetrakis(carbamoylmethyl)-1,4,7,10- tetraazacyclododecane) and a GRPR-targeted antagonist.
To determine the Recommended Phase 2 Dose (RP2D) of ²¹²Pb-DOTAM-GRPR1
Incidence of DLTs.
To assess the safety and tolerability of 212Pb-DOTAM-GRPR1.
Measured as Incidence and severity of TEAEs and TESAEs.
To assess the safety and tolerability of 203Pb-DOTAM-GRPR1.
Measured as Incidence and severity of TEAEs and TESAEs.
To assess PK of ²¹²Pb-DOTAM-GRPR1
212Pb-DOTAM-GRPR1 radioactivity concentration as a function of time in whole blood, plasma and urine
To evaluate the preliminary antitumor activity of 212Pb-DOTAM-GRPR1.
ORR by RECIST1.1, DOR, PFS by Investigator assessment and OS.
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