List of drugs by year of discovery


The following is a table with drugs, organized by their year of discovery.
Naturally occurring chemicals in plants, including alkaloids, have been used since pre-history. In the modern era, plant-based drugs have been isolated, purified and synthesised anew. Synthesis of drugs has led to novel drugs, including those that have not existed before in nature, particularly drugs based on known drugs which have been modified by chemical or biological processes.

Antiquity

60th millennium BC

Archaeological evidence indicates that the use of medicinal plants dates back to the Paleolithic age, these traditions were shared and transmitted by shamans since approximately 60,000 years ago.

4th millennium BC

In ancient Egypt, herbs are mentioned in Egyptian medical papyri, depicted in tomb illustrations, or on rare occasions found in medical jars containing trace amounts of herbs. Medical recipes from 4000 BC were for liquid preparations rather than solids. In 4th millennium BC is named Soma and Haoma but is not clear what were the ingredients to prepare them.

3rd millennium BC

DiscoveryName of drugActive ingredients
2,700 BCCannabis sativaTetrahydrocannabinol and cannabidiol.
2,700 BCMandragora officinarumAtropine and scopolamine, scopine, cuscohygrine, apoatropine, belladonnines and non-alkaloid constituents including sitosterol and scopoletin.
2,700 BCRhubarbAnthraquinones, which are cathartic and laxative. Stilbenoids, which may lower blood glucose levels. Flavanol glucosides which may be cytoprotective.

2nd millennium BC

Around 1600 BC was written Edwin Smith Papyrus, it describes the use of many herbal drugs, around 1550 BC was written the most important medical papyri of ancient Egypt, the Ebers Papyrus, it covers more than 700 drugs, mainly of plant origin. The first references to pills were found on papyruses in ancient Egypt, and contained bread dough, honey or grease. Medicinal ingredients, such as plant powders or spices, were mixed in and formed by hand to make little balls, or pills. The papyri also describe how to prepare herbal teas, poultices, ointments, eye drops, suppositories, enemas, laxatives, etc. Aloe vera was used in the 2nd millennium BC.

1st millennium BC

In Greece Theophrastus of Eresos wrote in the 4th c. B.C. Historia Plantarum Seeds likely used for herbalism have been found in archaeological sites of Bronze Age China dating from the Shang Dynasty. Over a hundred of the 224 drugs mentioned in the Huangdi Neijing, an early Chinese medical text, are herbs. Herbs also commonly featured in the medicine of ancient India, where the principal treatment for diseases was diet.
Opioids are among the world's oldest known drugs. Use of the opium poppy for medical, recreational, and religious purposes can be traced to the 4th century B.C., when Hippocrates wrote about it for its analgesic properties, stating, "Divinum opus est sedare dolores."
Year of discoveryName of the drugActive ingredients
1st millennium BCHyoscyamus nigerTropane alkaloids.
600 B.C.Glycerol, producedGlycerol
300 B.C.OpiumPhenanthrenes. Morphine binds to and activates mu opioid receptors and is analgesic. Opium also contains isoquinolines.

1st Century AD

In ancient Greece, pills were known as katapotia. Pliny the Elder, who lived from 23–79 AD, first gave a name to what we now call pills, calling them pilula. Pliny also wrote Naturalis Historia a collection of 38 books and the first pharmacopoea.
Pedanius Dioscorides wrote De Materia Medica ; this book dominated the area of drug knowledge for some 1500 years until the 1600s.
Jojoba was used in the 1st millennium AD.

2nd Century AD

wrote more than, also use terra sigillata with kaolinite and goats blood to produce tablets.

Post-classical to Early modern

Drugs developed in the post-classical or early modern eras.

6th-11th Century AD

In 754, during Abbasid Caliphate were formed the first pharmacies in Baghdad.
In middle age ointments were a common dosage form.
Year of discoveryName of the drugActive ingredients
10th centuryCoffeeCaffeine
Beta carboline

11th Century

Avicenna separates Medicine and Pharmacy, in 1025 published his book The Canon of Medicine, an encyclopedia of medicine formed by five books. Drugs mentioned by Avicenna include agaric, scammony and euphorbium. The latex of Euphorbia resinifera contains Resiniferatoxin, an ultra potent capsaicin analog. Desensitization to resiniferatoxin is tested in clinical trials to treat neuropathic pain.
Year of discoveryName of the drugActive ingredients
Before 1025AgaricMuscimol, muscarine, ibotenic acid
Before 1025Scammony
Before 1025EuphorbiumResiniferatoxin

16th Century

expounded the concept of dose response in his Third Defense, where he stated that "Solely the dose determines that a thing is not a poison." This was used to defend his use of inorganic substances in medicine as outsiders frequently criticized Paracelsus' chemical agents as too toxic to be used as therapeutic agents. Paracelsus discovered that the alkaloids in opium are far more soluble in alcohol than water. Having experimented with various opium concoctions, Paracelsus came across a specific tincture of opium that was of considerable use in reducing pain. He called this preparation laudanum.
For over a thousand years South American indigenous peoples have chewed Erythroxylon coca leaves, which contain alkaloids such as cocaine. Coca leaf remains have been found with ancient Peruvian mummies. There is also evidence coca leaves were used as an anesthetic. In 1569, Spanish botanist Nicolás Monardes described the indigenous peoples' practice of chewing a mixture of tobacco and coca leaves to induce "great contentment":
Year of discoveryName of the drug
Before 1569Erythroxylon coca leaves
16th centuryLaudanum

18th Century

In 1778 John Mudge created the first inhaler devices. In 1747, James Lind, surgeon of HMS Salisbury, conducted the first clinical trial ever recorded, on it he study how citrus fruit were capable of cure scurvy.

Modern

19th Century

In the 1830s chemist Justus von Liebig begin the synthesis of organic molecules, stating that "The production of all organic substances no longer belongs just to living organisms." In 1832 produced chloral hydrate, the first synthetic sleeping drug. In 1833 French chemist Anselme Payen was the first to discover an enzyme, diastase. In 1834, François Mothes and Joseph Dublanc created a method to produce a single-piece gelatin capsule that was sealed with a drop of gelatin solution. In 1853 Alexander Wood was the first physician that used hypodermic needle to dispense drugs via Injections. In 1858 Dr. M. Sales Giron invented the first pressurized inhaler.
Amphetamine was first synthesized in 1887 in Germany by Romanian chemist Lazăr Edeleanu who named it phenylisopropylamine; its stimulant effects remained unknown until 1927, when it was independently resynthesized by Gordon Alles and reported to have sympathomimetic properties. Shortly after amphetamine, methamphetamine was synthesized from ephedrine in 1893 by Japanese chemist Nagai Nagayoshi. Three decades later, in 1919, methamphetamine hydrochloride was synthesized by pharmacologist Akira Ogata via reduction of ephedrine using red phosphorus and iodine.

20th Century

In 1901 Jōkichi Takamine isolated and synthesized the first hormone, Adrenaline. In 1907 Alfred Bertheim synthesized Arsphenamine, the first man-made antibiotic. In 1927 Erik Rotheim patented the first aerosol spray can. In 1933 Robert Pauli Scherer created a method to develop softgels.
William Roberts studies about penicillin were continued by Alexander Fleming, who in 1928 concluded that penicillin had an antibiotic effect. In 1944 Howard Florey and Ernst Boris Chain mass-produced penicillin. In 1948 Raymond P. Ahlquist published his seminal work where divided adrenoceptors into α- and β-adrenoceptor subtypes, this allowed a better understanding of drugs mechanisms of action.
In 1987, after Montreal Protocol, CFC inhalers were phased out and HFA inhalers replace them. In 1987 CRISPR technique was discovered by Yoshizumi Ishino that in the next century would be used for genome editing.
Year of discoveryName of the drugYear when the synthesis mechanism was developedYear that was PatentedGovernmental approvalPatented expired
1901AdrenalineJōkichi Takamine, 190119011901N/A
1906OxytocinDiscovered by Henry Hallett Dale, synthesized by Vincent du Vigneaud in 195219251926N/A
1907ArsphenamineAlfred Bertheim, 1907N/AN/AN/A
1908PhenytoinHeinrich Biltz, 1908N/AN/AN/A
1912Vitamin CTadeusz Reichstein, 1933N/AN/AN/A
1912PhenobarbitalFischer and Mering Synthesis, 1912191219121932
1915ThyroxineIsolated by Edward Calvin Kendall, 191519151915N/A
1918ErgotamineIsolated by Arthur Stoll, Sandoz, 1918191819181938
1920Metamizole1920N/AN/AN/A
1921InsulinFrederick Grant Banting, 192119211921N/A
1927LevothyroxineHarington and Barger Synthesis, 1927N/A1927
1928PenicillinAlexander Fleming, 192819281928Never patented
1932SulfanilamidePaul Josef Jakob Gelmo, 1908N/AN/A1938
1932ProntosilGerhard Domagk, Josef Klarer and Fritz Mietzsch 1932N/AN/A1938
1935CortisoneIsolted by Philip Showalter Hench and Edward Calvin Kendall, 193519351935N/A
1935Tetracaine1935193519351955
1935Methylphenobarbital1935193519351955
1935Dapsone1935193519351955
1940Dicoumarol 1940, extracted from Melilotus194019401960
1946Isosorbide1946194619461966
1943LidocaineNils Löfgren, 1943194619491966
1938Lysergic acid diethylamide Albert Hofmann, Sandoz193819381958
1951Hydrocortisone1951195119511971
1951Imipramine1951195119571971
1952Acetazolamide1952195219521972
1954Fludrocortisone acetate1954195419541974
1955Prednisolone1955195519551975
1955Prednisone1955195519551975
1955ChlordiazepoxideLeo Sternbach, Hoffmann-La Roche, 1955195519551975
1956Methylprednisolone1956195619561976
1956Triamcinolone1956195619561976
1957Spironolactone1957195719571977
1957MepivacaineA. F. Ekenstam, 1957195719571977
1957Bupivacaine1957195719571977
1957Chlorothiazide1957195719571977
1958Dexamethasone1958195819581978
1958Betamethasone1958195819581978
1958Clozapine1958195819581978
1958Triamcinolone acetonide 1958195819581978
1959Hydrochlorothiazide1959195919591979
1959Clortalidone1959195919591979
1960FentanylPaul Janssen, Janssen Pharmaceutica 1960196019691980
1961Mefenamic acidClaude Winde, Parke-Davis 1961196119691981
1961IbuprofenBoots Group, 1961196119691981
1961FlurbiprofenBoots Group, 1961196119691994
1962Trimethoprim19621982
1962FurosemideCalvin L. Stevens, Parke-Davis 196219621982
1962KetamineCalvin L. Stevens, Parke-Davis 196219621982
1962PiroxicamPfizer 196219621992
1962MeloxicamPfizer 19621962Not for use in humans
1962BeclometasoneDavid Jack, 196219621982
1963DiazepamLeo Sternbach, 1963196319631983
1963Indometacin1963196319651983
1963Flufenamic acidParke-Davis, 1963196319651983
1963Ropivacaine1963196319631983
1964Meclofenamic acidParke-Davis, 1963196319651983
1964PropranololJames Black, 19641964
1964ClonazepamLeo Sternbach, 1964196419641984
1964Triamterene1964196419641984
1964Tetrahydrocannabinol 196419641964N/A
1966Salbutamol David Jack, Allen & Hanburys, 196619661986
1967Amiloride1964196419641984
1968Prilocaine196819681968N/A
1970CiclosporinB. Vithal Shetty, 19711982
1971MetolazoneB. Vithal Shetty, 19711971
1971CimetidineJames Black, 19711971
1971MupirocinIsolated in 19711971
1971EtidocaineIsolated in 19711971
1973DiclofenacSynthesized by Alfred Sallmann and Rudolf Pfister in 197319731993
1973Budesonide197319731993
1974SulfentanilJanssen Pharmaceutica, 19741994
1974CarfentanilJanssen Pharmaceutica, 19741994
1976Ipratropium bromide197619761996
1976Naproxen197619761996
1977RanitidineJohn Bradshaw, Allen & Hanburys, 19771981
1977PropofolJohn Bradshaw, Allen & Hanburys, 19771981
1977TramadolGrünenthal GmbH, 197719771997
1981Verapamil198119811997
1985Salmeterol David Jack, Allen & Hanburys, 198519852005
1984SumatriptanDavid Jack, 198419842006
1987OndansetronDavid Jack, 198719902006
1989Ketorolac198919892009
1993Fluticasone propionateDavid Jack, 199319932004
1993KetoprofenJames W. Young, William J. Wechter and Nancy M. Gray in 199319932003
1993Celecoxib199319932003
1993Rofecoxib199319932003
1995Parecoxib1995Not approved2015
1996Lopinavir2000-
1997Mometasone furoate 199719972017
1997Eletriptan199720022017
1998Ropivacaine1998199819982008
1998Leflunomide199819982008

21st Century

begins with the first complete sequences of individual human genomes by Human Genome Project, on February 12, 2001, this allowed a switch in drug development and research from the traditional way of drug discovery that was isolating molecules from plants or animals or create new molecules and see if they could be useful in treatment of illness in humans, to pharmacogenomics, that is the study and knowledge of how genes respond to drugs. Another field beneficed by Human Genome Project is pharmacogenetics, that is the study of inherited genetic differences in drug metabolic pathways which can affect individual responses to drugs, both in terms of therapeutic effect as well as adverse effects.
Humane genome study also allowed to identify which genes are responsible of illness, and to develop drugs for rare diseases and also treatment of illness through gene therapy. In 2015 a simplified form of CRISPR edition was used in humans with Cas9, and also was used an even more simple method, CRISPR/Cpf1 that prevent genetic damage from viruses. These advances are improving personalized medicine and allowing precision medicine.
Year of discoveryName of the drugYear when the synthesis mechanism was developedYear that was PatentedGovernmental approvalPatented expiryDrug type *
2000Bevacizumab20042024MA
2001Valdecoxib2016N/ASM
2001Etoricoxib2016N/ASM
2003Alirocumab20152035MA
2006Linagliptin20112031SM
2007Apixaban20122032SM
2007Alectinib20142014SM
2007Sofosbuvir2007, Raymond F. Schinazi.N/AN/AN/ASM
2007BevirimatSM
2012Ivacaftor20122032SM
2013Vilanterol20132033SM
2014Evolocumab20152035MA
2014Umeclidinium bromide 20142034SM
2014Tisagenlecleucel20172037ACT

* MA = Monoclonal antibody
SM = Small molecule
ACT = Adoptive cell transfer