Dose Escalation Study of NKP-1339 to Treat Advanced Solid Tumors

NKP-1339 is a novel GRP78 targeted ruthenium based anti-cancer compound which is
intravenously administered. GRP78 is a key regulator of misfolded protein processing, which
is unregulated in cancer cells. In nonclinical anti-tumor studies, NKP-1339 showed activity
against many tumor types, including those resistant to platinum and other standard
anti-cancer agents. This Phase I trial evaluates the safety, tolerability, maximum tolerated
dose, pharmacokinetics, and pharmacodynamics of NKP-1339.

Inclusion Criteria:

- Patients ≥ 18 years with histologically or cytologically confirmed advanced solid
tumors refractory to standard therapies who have signed an IRB approved Informed
Consent Form (ICF).

- ECOG PS 0 or 1.

- Adequate hematologic, hepatic and renal function

- Minimum life expectancy ≥ 12 weeks

Exclusion Criteria:

- No supplemental Iron, i.e., therapeutic or as part of a multivitamin regimen.

- No chemotherapy, immunotherapy, or radiotherapy for < 4 weeks, BMTs < 9 months or
major surgery < 3 weeks.

- No symptomatic central nervous system metastases. No primary brain tumors or known
brain metastasis unless clinically stable and on stable or reducing dose of steroids.

- No evidence of ischemia, MI within the past 6 months, or other significant
abnormality on ECG.

- No clinically significant active infection including HIV, hepatitis B, or hepatitis
C.

- No Peripheral neuropathy ≥ Grade 2