2.

LITERATURE REVIEW
 2. LITERATURE REVIEW

2.1 REVIEW OF LITERATURE24-41

Non Official Method
2.1 Literature of Selumetinib
DRUG TITLE AUTHOR BRIEF INTRODUCTION

selumetinib Determination of Paul Severin, Robust and sensitive LC–

elumetinib, N- smethyl Christopher MS/MS assays for the
selumetinib and Bailey, Meng
quantification of selumetinib
elumetinib amide in Chen
human biological and two of its metabolites
amples by LC–MS/MS were validated in human
biological matrices and are
being used to support the
clinical development
program.

selumetinib Novel LC–MS/MS Ramakrishna high calibration standard

method for the R Voggu, (2000 ng/ml). Carryover was
determination of Theodore S
observed less than 5% of
Selumetinib Brus, Chineta
(AZD6244) in whole T Barksdale LLOQ signal.
blood ollected with
olumetric absorptive LQC (6.00 ng/ml), MQC
microsampling (800 ng/ml), and HQC (1600
ng/ml)

Selumetinib recoveries were

104.1, 101.6 and 103.4%.

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 2. LITERATURE REVIEW

Tyrosine Simultaneous and Yanping Liu,, Wavelength: 283 nm.

Kinase Rapid Determination Hua Liu,
Inhibitors of Six Tyrosine Kinase Zhewei Xia Column: Agilent Zorbax SB-
Inhibitors in Patients C18 reversed-phase column
with Non-Small Cell
(2.1mm× 100 mm, 3.5 μm,
Lung Cancer
Using HPLC-MS/MS Agilent, USA)

Mobile phase: 0 0.1% formic

acid in water (phase A) and
0.1% formic acid in
acetonitrile (phase B)

Flow rate : 0.3 ml/min

Linear correlation
coefficients were >0.990

Tyrosine A New HPLC–UV Elisa Pirro, Wavelength: 267 nm.

Kinase Validated ethod for Silvia De
Inhibitors Therapeutic Drug Francia, Column: RP-C18
Monitoring of Francesca De LiChroCART 250-4
Tyrosine Kinase Martino1 LiChrospher 100 RP 18, 5μ,
Inhibitors in Leukemic VWR
Patients
Mobile phase: 40% solvent
A, 20%

methanol, and 40%

acetonitrile. Solvent A
consisted of water (72.5%),
methanol, (25%), and
triethylamine (2.5%).

Flow rate : .0.9 ml/min

intra-day and inter-day

precision: 2.5 and 13.3%;

accuracy: 13.9%;

Tyrosine Stimulation of Takaki Serine/threonine kinase

Kinase ltraviolet-induced Hiwasaa, inhibitors, K252a,
Inhibitors apoptosis of human Yoshiko
staurosporine and
broblast UVr-1 cells Araseb,
by tyrosine kinase Zheng Chena GF109203X, rather

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 2. LITERATURE REVIEW

inhibitors suppressed the

ultravioletinduced DNA
cleavage.
Tyrosine The Quantitative Sandra Column: Hyperclone 3u
Kinase Analysis Of Tyrosine Roche, ODS C18 100X2.0mm
Inhibitors Kinase Inhibitor evels Martin
In Biological Samples Clynes, Mobile 10mM ammonium
By LC-MS Robert O’ formate buffer (pH4)-
Connor acetonitrile

Flow rate : 200 ml/min

Tyrosine Development and Lutz Götze , Column: Kinetex C18

Kinase clinical application of Axel Hegele , column (50×4.6 mm, 2.6 μ,
Inhibitors a LC-MS/MS method Stephan Phenomenex)
for simultaneous Klaus
determination of Metzelder Mobile phase water
various tyrosine kinase acetonitrile containing 1%
inhibitors in human formic acid with 10 mM
plasma ammoniumformiate

Flow rate : 0.3 ml/min

The calibration range was

10–1000 ng/mL for sunitinib
and 50–5000 ng/mL

Coefficients: of
determination ≥0.99

Tyrosine A new HPLC-UV Pirro E; De Wavelength: 267 nm.

Kinase validated method for Francia S; De
Inhibitors therapeutic drug Martino Column: C18 RP column
monitoring of tyrosine
kinase inhibitors in (LiChroCART® 250-4
leukemic patients LiChrospher® 100 RP 18,

R2: 0.8972

Mobile phase: 40% solvent

A, 20% methanol, 40%
acetonitrile. Solvent A
consisted of Water (72.5%)
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 2. LITERATURE REVIEW

Methanol (25%) and

riethylamine (2.5%).

Flow rate 0.3 ml/min

Tyrosine ICH Guidelines- Nasr Y. Wavelength: 270 nm.

Kinase compliant HPLC-UV Khalil,
Inhibitor Method for Ibrahim A. Column: Nucleosil CN with
Pazopanib Pharmaceutical Darwish, dimensions (i.d. 250 × 4.6
Quality Control and Munif F. mm and particle size 5 μm)..
Therapeutic Drug Alshammari Mobile phase :
Monitoring of the acetonitrile:100 mM sodium
Multi-targeted acetate buffer (pH 4.5);
Tyrosine Kinase 40:60, v/v.
Inhibitor Pazopanib
flow rate of 1.0 mL/min

(LOD and LOQ) were 0.27

and 0.82 μg mL–1

Nintedanib Facile And Sensitive Kohei Wavelength: 390 nm

Hplc-Uv Method For Togami,
Determination Of Kenta Column: ightysil RP-18 GP
Nintedanib In Rat Fukuda, II ODS column (250 × 3.0
Plasma Kotaro mm, length by inner
Yamaguchi diameter, 5-μm particle size)

Mobile phase 20 mmol

phosphate buffer (pH 3.0)
and acetonitrile (7:3, v/v)

flow rate of 0.6 mL/min

concentration in this method

was 12.5–400 ng/ml,

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 2. LITERATURE REVIEW

Imatinib Validation and Álvaro Corral Wavelength: 263 nm

Comparison of Two Alaejos ·
Analytical Methods Silvia Column : Luna Omega C18
for Imatinib Jiménez column (1.6 μm; 2.1 mm x
Therapeutic Drug Cabrera 50 mm, Phenomenex
Monitoring Company)

mobile phase used for elution

consisted of a mixture 70/30
of potassium phosphate 0.02
M (pH = 3.2) and
acetonitrile.

flow rate of 0.5 mL/min

linear over the range 500–

2750 ng/ml

(r = 0.996) and 500–3000

ng/ml (r = 0.999)

Baricitinib Development and Santosh V. Wavelength: 250 nm.

Validation of UV Gandhi,
Spectroscopic Method Barkha G. concentrations 10-60 μg/ml
for Estimation of Kapoor
y=0.031 x+0.080
Baricitinib.
R² = 0.993

Pazopanib Development and Vanesa Wavelength:260 nm.

Validation of an Escudero-
HPLC-UV Method for Ortiz, Juan J. Column: Ultrabase C18
Pazopanib Pérez-Ruixo, column
Quantification in and Belén
Human Plasma and Valenzuela Mobile phase: vol/vol
Application to Patients proportion of 47:53 of
With Cancer in ammonium acetate (pH, 7;
Routine Clinical 0.02 mol/L) and
Practice cetonitrile/methanol (70:30,
vol/vol)

Flow rate : 1.0 ml/min

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 2. LITERATURE REVIEW

limit of detection and the

lower limit of quantification
were 0.2 and 0.5 mcg/mL,

sunitinib Development and Benoit Wavelength: 431nm.

validation of an Blanchet,
HPLC-UV-visible Carole Column: cyanopropyl
method for sunitinib Saboureau, column
quantification in Anne Sophie
Mobile phase: ammonium
human plasma Benichou
acetate buffer (20 mM; pH
6.8):acetonitrile (55:45,v/v).

Flow rate : 1.0 ml/min

calibration was linear in the

range 20–200 ng/mL

Dasatinib, Analytical Methods P. Ravi Column: Gemini C18

Lapatinib, For Determination Of Sankar, A. column (50 × 2.0 mm i.d.,
Imatinib, Different Members Of Bhavani 5.0 μm particle size
Sorafenib, FDA approved Sailu, M. M.
Nintedanib, Tyrosine Kinase Eswarudu, M. vol/vol proportion of 47:53
Sunitinib And Inhibitors Like Nithya Satya, of ammonium acetate,
Pazopanib Dasatinib, Lapatinib, acetonitrile/methanol (70:30,
Imatinib, Sorafenib, vol/vol)
Nintedanib, Sunitinib linear range from 20.0 to
And Pazopanib: A 10,000 ng/mL
Review

alectinib, Development and Hadir M. column : Waters

ceritinib, and validation of UPLC– Mahera,, BEHTMC18 column
crizotinib MS/MS method for Aliyah
thesimultaneous Almomena, mobile phase: amixture of
quantification of Nourah Z. acetonitrile/water containing
anaplastic lymphoma Alzomana 0.1 % formic acid (70: 30,
kinaseinhibitors, v/v)
alectinib, ceritinib, and The flow rate: 0.2 mL/min
crizotinib in Wistar rat
plasma withapplication concentration ranges of
to bromelain-induced 2−200, 0.4−200, and
pharmacokinetic 4.0−200ng/mL
interaction

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 2. LITERATURE REVIEW

Tyrosine Chemometrics M Wavelength: 277nm.

Kinase Assisted Rp-Hplc Rajavardhan
Method Development Reddy, Column: Phenomenex
For The Separation Of Kirtimaya Enable C18 column (15×4.6
Second Generation Mishra, mm id, 5μm particle size)
Tyrosine Kinase P.K.Manna, R
Mobile phase: MeOH: 60-
Inhibitors In Bulk Suresh
70%, pH: 2-2.5
Drugs And
Pharmaceutical Flow rate : 0.3-0.8ml/min
Formulations
R2 were more than 0.9258

retention times of 2.7, 3.2,

and 6.0 minutes

Tyrosine A stability indicating Ramana Wavelength: 230 nm.

Kinase method development Reddy
and validation for Gopireddy, Column: YMC Triart C-18
separation (150 4.6 mm, 3.0 mm)
Arthanareesw
of process related
impurities and ari
Mobile phase water pH: 3.5
characterization of Maruthapillai
± 0.05 adjusted with diluted
unknown
Ortho phosphoric acid) as a
impurities of tyrosine
kinase inhibitor buffer and acetonitrile in a
Nilotinib by RP- ratio of 85:15 (%v/v)
HPLC, NMR respectively as mobile phase-
spectroscopy and ESI- A, and 10 mM NH4H2PO4
MS buffer, acetonitrile and
methanol in a ratio of
20:27.5:52.5 (%v/v/v)

Flow rate : 1ml/min

Tyrosine Development and G. Sowjanya, Wavelength: 254 nm.

Kinase Validation of a M. Mathrusri
Inhibitor Stability Indicating Annapurna Column: C18 column (250
RP-HPLC Method for and A. mm × 4.6 mm i.d., 5 μm
the Determination of Venkata particle size)
Nilotinib (A Tyrosine Sriram
Kinase Inhibitor)
Mobile phase water:
acetonitrile: acetic acid
(20:80: 0.03, v/v)

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 2. LITERATURE REVIEW

Flow rate : 1ml/min

R2 = 0.9997

y = 169118x - 11095

Official method:
selumetinib Monograph IP Column: USP

mobile phase :

flow rate:

Wavelength:

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