* Information from four completed trials. Data collection ongoing.
** Information obtained from Erbitux® and Vectibix® product labels
- Affinity-optimised: activity of Nimotuzumab is concentrated at tumors
- Nimotuzumab does not cause severe adverse reactions and no grade 3-4 skin rash from the treatment
Excellent safety profiles
Nimotuzumab (TheraCIM® h-R3) is a humanised antibody with a larger proportion of human sequence resulting in a low anti-idiotypic response. The affinity to EGFR of Nimotuzumab is of a lower magnitude than other mAbs. Also, Nimotuzumab has been obtained by humanising a murine antibody elicited against EGFR of human placenta and not of cultured cells.
Severe acne-like skin rash is a common toxicity seen with the use of anti-EGFR agents and often leads to discontinuation of therapy. 33 Rash has been seen in 88% of patients treated with cetuximab in combination with irinotecan, and in 90% of patients treated with cetuximab used alone. In a phase II trial with panitumumab, 100% of patients had rash. In contrast, skin rash has rarely been reported with the use of Nimotuzumab in patients with advanced epithelial tumours. Nimotuzumab produced complete response in 11 out of 16 patients (68.75%) with advanced stage head and neck cancer without causing a skin rash in any of the cases.33 The relatively lower affinity of Nimotuzumab for EGFR, which is 10- to 100-fold less than that of cetuximab, panitumumab or matuzumab might explain the superior safety profile of Nimotuzumab among anti-EGFRs.
Beneficial pharmacokinetic profile
No loading dose & lower dose requirement
In contrast with other anti-EGFR, Nimotuzumab does not require loading dose. The effective dose of Nimotuzumab is much lower than that of several other anti-EGFR agents. The optimum dose for management of unresectable head and neck squamous cell carcinoma (SCCHN) was found to be 200 mg weekly. Meanwhile, cetuximab is required in higher doses of 400 mg/m2 given as a loading dose, followed by 250 mg/m2. The high therapeutic index of TheraCIM® ensures excellent efficacy with minimal side effects.
Optimized affinity constant
The pharmacokinetic properties of Nimotuzumab are different from that of other anti-EGFR antibodies. Nimotuzumab has intermediate affinity (KD = 10-9 M) for EGFR. Intermediate affinity for EGFR is associated with an optimum effect which has high tumour uptake and low uptake in normal tissues. The maximum difference between the AUC for the tumour and normal tissue is achieved with intermediate affinity antibodies. Nimotuzumab shows maximum uptake and retention in tumour and rapid clearance from normal tissue.
Proven efficacy in various indications
Indications (approved in selected countries)