Inclusion Criteria:

1. Patient is male aged 18 years or older;

2. Histological, pathological, and/or cytological confirmation of adenocarcinoma of the
prostate;

3. Patients must have at least 1 metastatic lesion present on CT, MRI, or bone scan
imaging;

4. Patients must have progressive mCRPC based on at least 1 of the following criteria:

1. Serum/plasma PSA progression defined as increase in PSA greater than 25% and >2
ng/mL above nadir, confirmed by progression at 2 time points at least 3 weeks
apart

2. Soft-tissue progression defined as an increase ≥20% in the sum of the diameters
(SOD) (short axis for nodal lesions and long axis for non-nodal lesions) of all
target lesions based on the smallest SOD since treatment started or the
appearance of one or a new lesion

3. Progression of bone disease defined as the appearance of 2 or more lesions by
bone scan

5. Progression on prior treatment with ≥1 ARPI (abiraterone, apalutamide, darolutamide,
enzalutamide ) in nmCRPC, mHSPC or mCRPC;

6. PSMA-PET scan ([Ga-68]-PSMA-11 or [F-18]-DCFPyL) positive as determined by local
investigator;

1. At least 1 PSMA-PET positive lesion for prostate cancer

2. Uptake greater than the liver will be used as the reference for determining
PSMA-PET positivity and uptake less than or equal to the liver will be used as
the reference for determining PSMA-PET negativity

3. All lymph nodes that measure ≥25 mm in short axis on anatomic imaging must be
PSMA-PET positive

4. All bone metastases with soft tissue component(s) ≥10 mm in short axis must be
PSMA-PET positive (PSMA-negative osseous metastases without a soft tissue
component do not exclude patients)

5. All solid organ metastases (i.e., lung, liver, adrenal glands, etc.) ≥10 mm in
short axis must be PSMA-PET positive

7. Castrate levels of circulating testosterone (<1.7 nmol/L or <50 ng/dL);

8. Patients must have recovered to Grade ≤2 from all clinically significant toxicities
related to; prior therapies (i.e., prior ARPI, chemotherapy, PARPi, radioisotope or
immunotherapy, etc.)

9. Adequate organ function, independent of transfusion;

a. Bone marrow reserve

i. White blood cell (WBC) count ≥2.5 x 109/L OR absolute neutrophil count (ANC) ≥1.5
x 109/L ii. Platelets ≥100 x 109/L iii. Hemoglobin ≥80 g/L or ≥8 g/dL

b. Liver function

i. Total bilirubin ≤1.5 x institutional upper limit of normal (ULN). For patients
with known Gilbert's syndrome, ≤3.0 x ULN ii. ALT and AST ≤3.0 x ULN

c. Renal function

i. Creatinine clearance ≥50 mL/min based on Cockroft-Gault formula

d. Albumin ≥30 g/L

10. Human immunodeficiency virus-infected patients who are healthy and have a low risk
of acquired immunodeficiency syndrome-related outcomes are eligible;

11. ECOG performance status 0 or 1;

12. For patients who have partners who are pregnant or of childbearing potential: a
condom is required along with a highly effective contraceptive method during the
study and for 6 months after last study drug administration. Such methods deemed
highly effective include a) combined (estrogen and progestogen containing) hormonal
contraception associated with inhibition of ovulation, b) progestogen-only hormonal
contraception associated with inhibition of ovulation, c) intrauterine device (IUD),
d) intrauterine hormone-releasing system (IUS), e) bilateral tubal occlusion, f)
vasectomy, g) true sexual abstinence: when this is in line with the preferred and
usual lifestyle of the subject [periodic abstinence (e.g., calendar, ovulation,
symptothermal, post-ovulation methods), declaration of abstinence for the duration
of exposure to IMP, and withdrawal are not acceptable methods of abstinence].

13. Signed Informed Consent Form

Exclusion Criteria:

1. Prior PSMA-targeted radioligand therapy (i.e., [Lu-177]-PSMA-617);

2. A superscan defined as a bone scan that demonstrates markedly increased skeletal
radioisotope uptake relative to soft tissues in association with absent or faint
genitourinary tract activity;

3. Patients with a history of central nervous system (CNS) metastases must have
received therapy (surgery, radiotherapy, gamma knife) and be neurologically stable,
asymptomatic, and not receiving corticosteroids for the purposes of maintaining
neurologic integrity;

4. Patients with epidural disease, canal disease and prior cord involvement are
eligible if those areas have been treated, are stable, and not neurologically
impaired. For patients with parenchymal CNS metastasis (or a history or CNS
metastasis), baseline and subsequent radiological imaging must include evaluation of
the brain (MRI preferred or CT with contrast);

5. Symptomatic cord compression, or clinical radiologic findings indicative of
impending cord compression;

6. Any pre-existing symptoms, or concurrent severe and/or uncontrolled medical
conditions such as ureteral obstruction, which in the opinion of the investigator
would compromise safe participation in the [Lu-177]-PNT2002 EAP;

7. Not able to understand and comply with treatment instructions and requirements;