UGT1A1regorafenib

FOLFIRIirinotecan

UGT1A1
regorafenibFOLFIRI
irinotecan

20%~25%

40%

2012FDA

2013

FOLFOX(5-fluorouracil/

regorafenib

leucovorinoxaliplatin )

FOLFIRI(5-fluorouracil/
leucovorinirinotecan)

66

20

10%

bevacizumabcetuximab

(adenocarcinoma)

IIIB(CEA)

36.6 ng/mL

156

 JOURNAL OF KAOHSIUNG MEDICAL ASSOCIATION 2015. vol. 23, No.2

IIIB (T3N1aM0)

leucovorin 5-fluorouracil

CEA

irinotecan

KRAS wild-

2030 mg/m 2

type

290 mg/m2 (180, 210,

FOLFIRI (180 mg/

240, 260, 290 mg/m2)

m 2 dose of irinotecan)
2

UGT1A1

cetuximab 500 mg/m

FOLFIRI regimen

irinotecan

regorafenib

FOLFIRI

regorafenib (160

progression-free survival

mg daily for the first 21 days

of each 28-day cycle)

FOLFIRIregorafenib

(partial

(hand-foot skin

response)

reaction)

(1A
1B)CEA 708.09
ng/mL97.42 ng/mL

:
Irinotecan

FOLFIRI

7-ethyl-10-

regimenirinotecan

hydroxycamptothecin (SN-38)

UGT1A1 (uridine diphosphate

SN-38

glucuronosyItransferase)

UDP-glucuronosyltransferase

6/6 TA

(UGT)SN-

((TA)n repeat)

38GSN-38SN-38G

UGT1A1 genotyping

(glucuronidation)

irinotecan

irinotecan

UGT1A1 gene

180 mg/m

157

(TATA box sequences)

UGT1A1regorafenib
FOLFIRIirinotecan

SN-386TA

UGT1A1*28 allele

repeat(UGT1A1*1 allele, wild-

2012FDA2013

type)7TA repeats(UGT1A1*28
mutant)

FOLFOX

irinotecan

FOLFORIanti-

FOLFIRI

vascular endothelial growth

irinotecan

factoranti-epidermal growth

allele,

180 mg/m

factor receptor pathway

UGT1A1 genotyping

UGT1A1*1 allele

regorafenib (multikinase

1. : FOLFIRI(irinotecan) regorafenib
(A)(B)()(
)

158

 JOURNAL OF KAOHSIUNG MEDICAL ASSOCIATION 2015. vol. 23, No.2

inhibitor targeting angiogenic,

irinotecan

stromal, and oncogenic receptor

regorafenib

tyrosine kinases)Regorafenib

receptor tyrosine kinases

angiogenesis

oncogenesistumor growth/

1.Ocvirk J, Brodowicz T, Wrba F, et al.

proliferation signaling

Cetuximab plus FOLFOX6 or FOLFIRI

(The Phase III

in metastatic colorectal cancer:

Regorafenib Monotherapy for

CECOG trial. World J Gastroenterol.

Previously Treated Metastatic

2010;16(25):31333143.

Colorectal Cancer Trial)

2.Hurwitz H, Fehrenbacher L, Novotny

disease control rate

W, et al. Bevacizumab plus irinotecan,

progression-free survival time

fluorouracil, and leucovorin for

overall survival benefit

metastatic colorectal cancer. N Engl J

(41% versus 15%,

Med. 2004;350(23):23352342.

P=0.001; 1.9 versus 1.7 months,

3.Yeh YS, Huang ML, Chang SF, Chen

P=0.001; 6.4 versus 5.0 months;

C F, H u H M , Wa n g J Y. F O L F I R I

P=0.0052)

combined with bevacizumab as first-

line treatment for metastatic colorectal

cancer patients with hyperbilirubinemia

Irinotecan
SN-38UDP-

after UGT1A1 Genotyping. Med Princ

Pract. 2014;23(5):478481.

glucuronosyltransferase

4.Lu CY, Huang CW, Hu HM, et al.

SN-38G

Prognostic advantage of irinotecan

regorafenib

dose escalation according to uridine

(glucuronosyl transferase)

diphosphate glucuronosyltransferase

irinotecanregorafenib

1A1 (UGT1A1) genotyping in patients

with metastatic colorectal cancer

UGT1A1

treated with bevacizumab combined

FOLFIRI

with 5-fluorouracil/leucovorin with

159

UGT1A1regorafenib
FOLFIRIirinotecan

irinotecan in a first-line setting. Transl

Res. 2014;164(2):169176.

6.Grothey A, Van Cutsem E, Sobrero

A, et al. Regorafenib monotherapy for

5.Crona DJ, Keisler MD, Walko CM.

previously treated metastatic colorectal

Regorafenib: a novel multitargeted

cancer (CORRECT): an international,

tyrosine kinase inhibitor for

multicentre, randomised, placebo-

colorectal cancer and gastrointestinal

controlled, phase 3 trial. Lancet.

stromal tumors. Ann Pharmacother.

2013;381(9863):303312.

2013;47(12):16851696.
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