Nktr- (Not yet branded)

Antibody-Drug Conjugate

US Experimental IV 4 Clinical Trials
Topoisomerase I

Description

NKTR-102 is an antibody-drug conjugate that combines irinotecan with a polyethylene glycol polymer to create a long-acting topoisomerase I inhibitor for colorectal cancer treatment. The drug has been evaluated in Phase 1 and Phase 2 trials specifically for patients with metastatic colorectal cancer, including those with KRAS mutations who are irinotecan-naïve. Clinical trials have tested NKTR-102 both as monotherapy and in combination with cetuximab for refractory solid tumors and advanced colorectal cancer.

Mechanism of Action

NKTR-102 uses a proprietary polymer conjugation technology to deliver irinotecan in a sustained manner, allowing the active metabolite SN-38 to accumulate preferentially in tumor tissues. The polyethylene glycol carrier extends the drug's half-life and modifies its distribution, potentially improving the therapeutic index compared to conventional irinotecan by reducing peak concentrations while maintaining antitumor activity.

Molecular Targets

Side Effects

Diarrhea Neutropenia Fatigue Nausea Vomiting Abdominal pain Decreased appetite Dehydration

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT04616196 Phase 1
Archived
Study of NKTR 255 in Combination With Cetuximab in Solid Tumors
United States
NCT03435640 Phase 1
Archived
REVEAL Study of NKTR-262 in Combination With NKTR-214 and Nivolumab in Patients With Locally Advanced / Metastatic Solid Tumor Malignancies
United States
NCT00856375 Phase 2
Archived
NKTR-102 Versus Irinotecan in Patients With Second-Line, Irinotecan-Naïve, KRAS Mutant, Colorectal Cancer
United States, Belgium, Germany, India, Spain, United Kingdom
NCT00598975 Phase 2
Archived
NKTR-102 in Combination With Cetuximab in Patients With Refractory Solid Tumors (Phase 2a) and Metastatic or Locally Advanced Colorectal Cancer (Phase 2b)
United States